Temozolomide (Synonyms: 替莫唑胺; NSC 362856; CCRG 81045; TMZ)

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Temozolomide (NSC 362856) 是一种可透过血脑屏障的口服活性的 DNA 烷基化 (DNA alkylating) 剂。Temozolomide 也是一种促自噬 (autophagy) 和促凋亡剂 (apoptosis)。Temozolomide 对以低水平的 O6-烷基鸟嘌呤 DNA 烷基转移酶 (OGAT) 和功能失配修复系统为特征的肿瘤细胞有效。Temozolomide 具有抗肿瘤和抗血管生成作用。

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CAS No. : 85622-93-1

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Other Forms of Temozolomide:

Temozolomide-d₃ In-stock
Temozolomide (Standard) 询价

MCE 顾客使用本产品发表的 163 篇科研文献

Proliferation Assay

Cell Viability Assay

IHC

: Temozolomide purchased from MCE. Usage Cited in: Acta Pharm Sin B. 2024 May;14(5):2097-2118.; Temozolomide (TMZ) (25 mg/kg; i.p.; administered during the first 3 days of each week for 4 weeks during reperfusion) significantly reduces the levels of synaptic-associated proteins including synaptophysin, PSD95, and GAP43 in wild-type mice subjected to MCAO.

: Temozolomide purchased from MCE. Usage Cited in: Adv Sci (Weinh). 2024 May;11(19):e2309290. [Abstract]; Temozolomide (TMZ) (5 mg/kg; orally gavaged once daily for 4 weeks) increases the levels of pan Kla and H3K9la in BALB/C mice with GBM xenografts.

: Temozolomide purchased from MCE. Usage Cited in: Adv Sci (Weinh). 2024 Apr;11(15):e2306027. [Abstract]; Temozolomide (TMZ) (1.5 mg/kg; i.p., every other day for 12 days) combined with PANK4 knockdown significantly reduces the expression of the tumor proliferation marker Ki-67 in T98GRes xenograft mice.

: Temozolomide purchased from MCE. Usage Cited in: MedComm. 2023 Jun 19;4(4):e281. [Abstract]; Temozolomide (TMZ) (300 μM) increases the expression of DAPK1, cleaved caspase-3 (C-Caspase3), and cleaved PARP (C-PARP) while decreasing MIB1 protein levels in both U-87 MG and LN-229 cells, and this effect is enhanced when combined with Sanggenon C (SC) (HY-N0617) (10 μM).

: Temozolomide purchased from MCE. Usage Cited in: J Pharm Anal. 2023 May;13(5):514-522.; Temozolomide (TMZ; 10 μM; 24 h) enhances the Sunitinib-induced (3 μM; 24 h) expression of γ-H2Ax in T98G cells.

: Temozolomide purchased from MCE. Usage Cited in: J Pharm Anal. 2023 May;13(5):514-522.; Temozolomide (TMZ; 10 μM; 24 h) enhances the Sunitinib-induced (3 μM; 24 h) expression of γ-H2Ax in T98G cells.

: Temozolomide purchased from MCE. Usage Cited in: Oncogene. 2023 Apr;42(16):1308-1320. [Abstract]; Temozolomide (TMZ; 60 mg/kg, i.g.; 5 consecutive days) treatment individually can suppress tumor growth, and the combination of knockdown MAEA and TMZ treatment can significantly inhibit tumor growth in mice (Fig A-B).

: Temozolomide purchased from MCE. Usage Cited in: Front Cell Dev Biol. 2021 Feb 1:9:620883. [Abstract]; Analyses of Western blotting shows that Temozolomide (TMZ) treatment increases the expression of CD133, SOX2, OCT4, and NANOG, suggesting that TMZ treatment promotes glioma stem cells (GSCs) formation in GBM cells.

: Temozolomide purchased from MCE. Usage Cited in: Theranostics. 2020 Jul 25;10(21):9477-9494. [Abstract]; Temozolomide (TMZ) (10 μM; 14 d) synergistically inhibits proliferation in STS cell lines when combined with MK4827 (HY-10619) (0.5 μM; 14 d).

: Temozolomide purchased from MCE. Usage Cited in: Oncotarget. 2016 May 17;7(20):29116-30. [Abstract]; U87MG glioma cells, and GBM8401 glioma cells are treated with DMSO or 20, 40, 60, or 80 μM of Hono, Mag or Hono-Mag combination for 24 hours. After treatment, the survival rate is analyzed using MTT tests. The right panels show Temozolomide (TMZ)-treated glioma cells which are regarded as a positive control.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects^[1]^[2].

IC₅₀ & Target

DNA alkylator^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A 172	IC₅₀	6.5 x 10⁴ nM Compound: Temozolamide	Antiproliferative activity against human A172 cells after 5 days by MTT assay Antiproliferative activity against human A172 cells after 5 days by MTT assay	[PMID: 22608389]
A 172	IC₅₀	> 40 μM Compound: TMZ	Cytotoxicity against human A 172 cells assessed as cell viability measured after 96 hrs by XTT assay Cytotoxicity against human A 172 cells assessed as cell viability measured after 96 hrs by XTT assay	[PMID: 34507011]
A-375	IC₅₀	> 75 μM Compound: TMZ	Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 34795855]
A-431	IC₅₀	366 μM Compound: TEM	Antiproliferative activity in human A431 Cells after 72 hrs by SRB assay Antiproliferative activity in human A431 Cells after 72 hrs by SRB assay	[PMID: 28494256]
A2058	IC₅₀	35.5 μM Compound: 1, TMZ	Chemosensitization of human A2058 cells after 5 days by MTT assay Chemosensitization of human A2058 cells after 5 days by MTT assay	[PMID: 23895620]
A2780	IC₅₀	183 μM Compound: Temozolomide	Potentiation of growth inhibition of A2780 cells along with 10 uM NU1085 in experiment 2 Potentiation of growth inhibition of A2780 cells along with 10 uM NU1085 in experiment 2	[PMID: 11063605]
A2780	IC₅₀	188 μM Compound: Temozolomide	Potentiation of growth inhibition of A2780 cells along with 10 uM NU1085 in experiment 1 Potentiation of growth inhibition of A2780 cells along with 10 uM NU1085 in experiment 1	[PMID: 11063605]
A2780	IC₅₀	368 μM Compound: Temozolomide	Potentiation of growth inhibition of A2780 cells by compound alone in experiment 2 Potentiation of growth inhibition of A2780 cells by compound alone in experiment 2	[PMID: 11063605]
A2780	IC₅₀	525 μM Compound: Temozolomide	Potentiation of growth inhibition of A2780 by compound alone in experiment 1 Potentiation of growth inhibition of A2780 by compound alone in experiment 1	[PMID: 11063605]
A2780	IC₅₀	8.5 μM Compound: 1, TMZ	Chemosensitization of human A2780 cells after 5 days by MTT assay in presence of MGMT inactivator PaTrin2 Chemosensitization of human A2780 cells after 5 days by MTT assay in presence of MGMT inactivator PaTrin2	[PMID: 23895620]
A2780	IC₅₀	> 250 μM Compound: 1, TMZ	Chemosensitization of human A2780 cells after 5 days by MTT assay Chemosensitization of human A2780 cells after 5 days by MTT assay	[PMID: 23895620]
A2780	IC₅₀	> 250 μM Compound: 1, TMZ	Cytotoxicity against human A2780 cells after 5 days by MTT assay in presence of 10 uM MGMT inactivator Patrin2 Cytotoxicity against human A2780 cells after 5 days by MTT assay in presence of 10 uM MGMT inactivator Patrin2	[PMID: 24900418]
A549	IC₅₀	> 250 μM Compound: 1, TMZ	Cytotoxicity against human A549 cells after 5 days by MTT assay Cytotoxicity against human A549 cells after 5 days by MTT assay	[PMID: 24900418]
Astrocyte	EC₅₀	51.8 μM Compound: 3, TMZ	Cytotoxicity against Rattus norvegicus Sprague-Dawley (rat) astrocytes after 4 days by cresylecth violet-staining method Cytotoxicity against Rattus norvegicus Sprague-Dawley (rat) astrocytes after 4 days by cresylecth violet-staining method	10.1007/s00044-010-9356-8
Astrocyte	IC₅₀	> 1 x 10⁶ nM Compound: Temozolamide	Cytotoxicity against mouse primary astrocytes after 5 days by MTT assay Cytotoxicity against mouse primary astrocytes after 5 days by MTT assay	[PMID: 22608389]
B16-F10	IC₅₀	258 μM Compound: Temozolomide	Growth inhibition of mouse B16F10 cells after 72 hrs by MTT assay Growth inhibition of mouse B16F10 cells after 72 hrs by MTT assay	[PMID: 22809560]
B16-F10	IC₅₀	> 75 μM Compound: TMZ	Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 34795855]
B16-F10	IC₅₀	> 75 μM Compound: Temozolomide	Cytotoxicity against mouse B16F10 cells after 72 hrs by MTS assay Cytotoxicity against mouse B16F10 cells after 72 hrs by MTS assay	[PMID: 28602669]
C6	EC₅₀	16.5 μM Compound: 3, TMZ	Cytotoxicity against Rattus norvegicus (rat) C6 cells after 4 days by cresylecth violet-staining method Cytotoxicity against Rattus norvegicus (rat) C6 cells after 4 days by cresylecth violet-staining method	10.1007/s00044-010-9356-8
C6	EC₅₀	60.46 μM Compound: TMZ	Antiproliferative activity against rat C6 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against rat C6 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay	[PMID: 31978780]
C6	IC₅₀	34 μM Compound: Temozolomide	Cytotoxicity against rat C6 cells incubated for 48 hrs by MTT assay Cytotoxicity against rat C6 cells incubated for 48 hrs by MTT assay	[PMID: 23069682]
C6	IC₅₀	60.46 μM Compound: TMZ	Inhibition of cell proliferation of rat C6 cells assessed as cell viability after 72 hrs by sulforhodamine B assay Inhibition of cell proliferation of rat C6 cells assessed as cell viability after 72 hrs by sulforhodamine B assay	[PMID: 25442304]
C6	IC₅₀	> 30 μM Compound: TMZ	Antiproliferative activity against rat C6 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against rat C6 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 34656900]
COLO 205	IC₅₀	343 μM Compound: Temozolomide	Cytotoxicity of compound in COLO 205 cell line Cytotoxicity of compound in COLO 205 cell line	[PMID: 11063604]
CTX TNA2	IC₅₀	430.6 μM Compound: TMZ	Cytotoxicity against rat CTX TNA2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against rat CTX TNA2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32960603]
CTX TNA2	IC₅₀	486.9 μM Compound: TMZ	Cytotoxicity against rat CTX TNA2 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against rat CTX TNA2 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 32960603]
CTX TNA2	IC₅₀	666.4 μM Compound: TMZ	Cytotoxicity against rat CTX TNA2 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against rat CTX TNA2 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32960603]
DBTRG-05MG	IC₅₀	119.3 μM Compound: TMZ	Cytotoxicity against human DBTRG-05MG cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human DBTRG-05MG cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32960603]
DBTRG-05MG	IC₅₀	354.7 μM Compound: TMZ	Cytotoxicity against human DBTRG-05MG cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human DBTRG-05MG cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 32960603]
DBTRG-05MG	IC₅₀	973.9 μM Compound: TMZ	Cytotoxicity against human DBTRG-05MG cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human DBTRG-05MG cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32960603]
DLD-1	GI₅₀	> 500 μM Compound: 1; TMZ	Growth inhibition of human DLD1 cells harboring hMSH6 mutation Growth inhibition of human DLD1 cells harboring hMSH6 mutation	10.1039/C6MD00384B
DLD-1	IC₅₀	> 250 μM Compound: 1, TMZ	Cytotoxicity against human DLD1 cells after 5 days by MTT assay Cytotoxicity against human DLD1 cells after 5 days by MTT assay	[PMID: 24900418]
GL261	IC₅₀	> 100 μM Compound: TMZ	Cytotoxicity against mouse GL261 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Cytotoxicity against mouse GL261 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 30939350]
H4	IC₅₀	47.9 μM Compound: Temozolomide	Antiproliferative activity against human H4 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human H4 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38377560]
H4	IC₅₀	> 100 μM Compound: TMZ	Antiproliferative activity against human H4 cells after 48 hrs by MTT assay Antiproliferative activity against human H4 cells after 48 hrs by MTT assay	[PMID: 26651221]
HCT-116	GI₅₀	291 μM Compound: 1a; TMZ	Antiproliferative activity against MMR-deficient human HCT-116 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against MMR-deficient human HCT-116 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 37262998]
HCT-116	GI₅₀	> 500 μM Compound: 1; TMZ	Growth inhibition of human HCT116 cells harboring hMLH1 mutation Growth inhibition of human HCT116 cells harboring hMLH1 mutation	10.1039/C6MD00384B
HCT-116	IC₅₀	4.34 μM Compound: Temozolomide	Cytotoxicity against human HCT116 cells after 4 days Cytotoxicity against human HCT116 cells after 4 days	[PMID: 19800803]
HCT-116	IC₅₀	< 50 μM Compound: 157	Anticancer activity against human HCT-116 cells assessed as reduction in cell viability Anticancer activity against human HCT-116 cells assessed as reduction in cell viability	[PMID: 33445154]
HCT-116	IC₅₀	> 250 μM Compound: 1, TMZ	Chemosensitization of human HCT116 cells after 5 days by MTT assay Chemosensitization of human HCT116 cells after 5 days by MTT assay	[PMID: 23895620]
HCT-116	IC₅₀	> 250 μM Compound: 1, TMZ	Cytotoxicity against human HCT116 cells after 5 days by MTT assay Cytotoxicity against human HCT116 cells after 5 days by MTT assay	[PMID: 24900418]
HT-29	IC₅₀	951 μM Compound: Temozolomide	Cytotoxicity of compound in HT-29 cell line Cytotoxicity of compound in HT-29 cell line	[PMID: 11063604]
HT-29	IC₅₀	> 250 μM Compound: 1, TMZ	Cytotoxicity against human HT-29 cells after 5 days by MTT assay Cytotoxicity against human HT-29 cells after 5 days by MTT assay	[PMID: 24900418]
HaCaT	IC₅₀	> 75 μM Compound: TMZ	Cytotoxicity against human HaCaT cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human HaCaT cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 34795855]
HeLa	GI₅₀	> 50 μM Compound: TMZ	Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 to 48 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 to 48 hrs by MTT assay	[PMID: 24986661]
HepG2	IC₅₀	5.9 μM Compound: Temozolomide	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by CCK-8 assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by CCK-8 assay	[PMID: 37335557]
Hs 683	IC₅₀	47.18 μM Compound: Temozolomide	Antiproliferative activity against human Hs 683 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human Hs 683 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38377560]
Hs 683	IC₅₀	956 μM Compound: Temozolomide	Growth inhibition of human Hs683 cells after 72 hrs by MTT assay Growth inhibition of human Hs683 cells after 72 hrs by MTT assay	[PMID: 22809560]
K562	IC₅₀	156.1 μM Compound: TEM	Cytotoxic effect in K562 cells Cytotoxic effect in K562 cells	[PMID: 12951113]
LN-18	IC₅₀	3.9 x 10⁵ nM Compound: Temozolamide	Antiproliferative activity against human LN18 cells after 5 days by MTT assay Antiproliferative activity against human LN18 cells after 5 days by MTT assay	[PMID: 22608389]
LN-229	IC₅₀	54.08 μM Compound: Temozolomide	Antiproliferative activity against human LN-229 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human LN-229 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38377560]
LN-229	IC₅₀	67.81 μM Compound: TMZ	Cytotoxicity effect against human LN-229 cells assessed as cell growth inhibition incubated for 48 hrs by trypan blue exclusion assay Cytotoxicity effect against human LN-229 cells assessed as cell growth inhibition incubated for 48 hrs by trypan blue exclusion assay	[PMID: 34304559]
LN-229	IC₅₀	> 1000 μM Compound: TMZ	Anticancer activity against human LN-229 cells assessed as cell growth inhibition inhibition incubated for 3 days Anticancer activity against human LN-229 cells assessed as cell growth inhibition inhibition incubated for 3 days	[PMID: 37201660]
LN-229	IC₅₀	> 500 μM Compound: Temozolomide	Antiproliferative activity against human LN-229 cells assessed as inhibition of cell growth incubated for 68 hrs by CCK-8 assay Antiproliferative activity against human LN-229 cells assessed as inhibition of cell growth incubated for 68 hrs by CCK-8 assay	[PMID: 39213937]
LoVo	IC₅₀	595 μM Compound: Temozolomide	Cytotoxic potentiation of Topotecan (TP) by the compound in (human colorectal cancer LoVo cell line Cytotoxic potentiation of Topotecan (TP) by the compound in (human colorectal cancer LoVo cell line	[PMID: 12408707]
MCF7	IC₅₀	800 μM Compound: Temozolomide	Inhibitory concentration of compound against Mer+ breast tumor cell line MCF-7 Inhibitory concentration of compound against Mer+ breast tumor cell line MCF-7	[PMID: 11055348]
MDA-MB-231	IC₅₀	14.4 μM Compound: Temozolomide	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability by CCK-8 assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability by CCK-8 assay	[PMID: 37335557]
MDA-MB-238	IC₅₀	> 100 μM Compound: TMZ	Cytotoxicity against human MDA-MB-238 cells assessed as cell viability measured after 96 hrs by XTT assay Cytotoxicity against human MDA-MB-238 cells assessed as cell viability measured after 96 hrs by XTT assay	[PMID: 34507011]
MDA-MB-436	IC₅₀	120 μM Compound: TMZ	Growth inhibition of human MDA-MB-436 cells after 72 hrs by SRB assay Growth inhibition of human MDA-MB-436 cells after 72 hrs by SRB assay	[PMID: 24388690]
MDCK	IC₅₀	1000 μM Compound: TMZ	Cytotoxicity against carbonic anhydrase 9 knockdown MDCK cells assessed as reduction in cell viability after 72 hrs under hypoxic condition by Alamar blue assay Cytotoxicity against carbonic anhydrase 9 knockdown MDCK cells assessed as reduction in cell viability after 72 hrs under hypoxic condition by Alamar blue assay	[PMID: 27823879]
MDCK	IC₅₀	775 μM Compound: TMZ	Cytotoxicity against carbonic anhydrase 9 knockdown MDCK cells assessed as reduction in cell viability after 72 hrs under normoxic condition by Alamar blue assay Cytotoxicity against carbonic anhydrase 9 knockdown MDCK cells assessed as reduction in cell viability after 72 hrs under normoxic condition by Alamar blue assay	[PMID: 27823879]
MDCK	IC₅₀	> 1000 μM Compound: TMZ	Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability after 72 hrs under hypoxic condition by Alamar blue assay Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability after 72 hrs under hypoxic condition by Alamar blue assay	[PMID: 27823879]
MDCK	IC₅₀	> 1000 μM Compound: TMZ	Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability after 72 hrs under normoxic condition by Alamar blue assay Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability after 72 hrs under normoxic condition by Alamar blue assay	[PMID: 27823879]
NCI	IC₅₀	100 μM Compound: 1	Antitumor activity against human NCI breast cancer cell line panel Antitumor activity against human NCI breast cancer cell line panel	[PMID: 15615536]
NCI	IC₅₀	100 μM Compound: 1	Antitumor activity against human NCI colon cancer cell line panel Antitumor activity against human NCI colon cancer cell line panel	[PMID: 15615536]
NCI	IC₅₀	100 μM Compound: 1	Antitumor activity against human NCI prostate cancer cell line panel Antitumor activity against human NCI prostate cancer cell line panel	[PMID: 15615536]
NCI	IC₅₀	79 μM Compound: 1	Antitumor activity against human NCI leukemia cell line panel Antitumor activity against human NCI leukemia cell line panel	[PMID: 15615536]
NCI	IC₅₀	93 μM Compound: 1	Antitumor activity against human NCI CNS cancer cell line panel Antitumor activity against human NCI CNS cancer cell line panel	[PMID: 15615536]
NCI	IC₅₀	98 μM Compound: 1	Antitumor activity against NCI human melanoma cell line panel Antitumor activity against NCI human melanoma cell line panel	[PMID: 15615536]
NCI	IC₅₀	98 μM Compound: 1	Antitumor activity against human NCI renal cancer cell line panel Antitumor activity against human NCI renal cancer cell line panel	[PMID: 15615536]
NCI-H1299	IC₅₀	> 100 μM Compound: TMZ	Cytotoxicity against human NCI-H1299 cells assessed as cell viability measured after 96 hrs by XTT assay Cytotoxicity against human NCI-H1299 cells assessed as cell viability measured after 96 hrs by XTT assay	[PMID: 34507011]
Non-small cell lung cancer cell line	IC₅₀	100 μM Compound: 1	Antitumor activity against human NCI non-small cell lung cancer cell line panel Antitumor activity against human NCI non-small cell lung cancer cell line panel	[PMID: 15615536]
PANC-1	IC₅₀	> 250 μM Compound: 1, TMZ	Cytotoxicity against human PANC1 cells after 5 days by MTT assay Cytotoxicity against human PANC1 cells after 5 days by MTT assay	[PMID: 24900418]
Panel NCI-60 (60 carcinoma cell lines)	GI₅₀	> 100 μM Compound: 1; TMZ	Growth inhibition of human NCI60 cells after 48 hrs by MTT assay Growth inhibition of human NCI60 cells after 48 hrs by MTT assay	10.1039/C6MD00384B
RG2	IC₅₀	106.7 μM Compound: TMZ	Cytotoxicity against rat RG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against rat RG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32960603]
RG2	IC₅₀	348.2 μM Compound: TMZ	Cytotoxicity against rat RG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against rat RG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 32960603]
RG2	IC₅₀	962.5 μM Compound: TMZ	Cytotoxicity against rat RG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against rat RG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32960603]
Raji	IC₅₀	175 μM Compound: 1	In vitro cytotoxicity against Raji cell line In vitro cytotoxicity against Raji cell line	[PMID: 7739008]
SF-268	GI₅₀	> 100 μM Compound: Temozolomide	Growth inhibition of human SF-268 cells measured after 24 to 72 hrs by SRB method Growth inhibition of human SF-268 cells measured after 24 to 72 hrs by SRB method	[PMID: 37163949]
SF-295	GI₅₀	> 100 μM Compound: Temozolomide	Growth inhibition of human SF-295 cells measured after 24 to 72 hrs by SRB method Growth inhibition of human SF-295 cells measured after 24 to 72 hrs by SRB method	[PMID: 37163949]
SF-539	GI₅₀	2.51 μM Compound: Temozolomide	Growth inhibition of human SF-539 cells measured after 24 to 72 hrs by SRB method Growth inhibition of human SF-539 cells measured after 24 to 72 hrs by SRB method	[PMID: 37163949]
SF-539	GI₅₀	> 100 μM Compound: Temozolomide	Growth inhibition of human SF-539 cells measured after 24 to 72 hrs by SRB method Growth inhibition of human SF-539 cells measured after 24 to 72 hrs by SRB method	[PMID: 37163949]
SH-SY5Y	IC₅₀	393 μM Compound: TMZ	Cytotoxicity against human SH-SY5Y cells using best fit nonlinear regression analysis Cytotoxicity against human SH-SY5Y cells using best fit nonlinear regression analysis	[PMID: 35044783]
SH-SY5Y	IC₅₀	512.62 μM Compound: TMZ	Cytotoxicity against human SH-SY5Y cells assessed as cell viability using raw interpretation method Cytotoxicity against human SH-SY5Y cells assessed as cell viability using raw interpretation method	[PMID: 35044783]
SH-SY5Y	IC₅₀	> 100 μM Compound: TMZ	Antiproliferative activity against human SH-SY5Y cells after 48 hrs by MTT assay Antiproliferative activity against human SH-SY5Y cells after 48 hrs by MTT assay	[PMID: 26651221]
SH-SY5Y	IC₅₀	> 50 μM Compound: Temozolomide	Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29789258]
SNB-19	GI₅₀	35.7 μM Compound: 1; TMZ	Growth inhibition of vehicle-transfected human SNB19 cells after 7 days by MTT assay Growth inhibition of vehicle-transfected human SNB19 cells after 7 days by MTT assay	[PMID: 30108945]
SNB-19	GI₅₀	45.6 μM Compound: 1; TMZ	Growth inhibition of empty vector transfected human SNB19 cells after 7 days by MTT assay Growth inhibition of empty vector transfected human SNB19 cells after 7 days by MTT assay	10.1039/C6MD00384B
SNB-19	GI₅₀	470 μM Compound: 1; TMZ	Growth inhibition of MGMT-transfected human SNB19 cells expressing MGMT after 7 days by MTT assay Growth inhibition of MGMT-transfected human SNB19 cells expressing MGMT after 7 days by MTT assay	[PMID: 30108945]
SNB-19	GI₅₀	526 μM Compound: 1; TMZ	Growth inhibition of MGMT-transfected human SNB19 cells after 7 days by MTT assay Growth inhibition of MGMT-transfected human SNB19 cells after 7 days by MTT assay	10.1039/C6MD00384B
SNB-19	GI₅₀	> 100 μM Compound: Temozolomide	Growth inhibition of human SNB-19 cells measured after 24 to 72 hrs by SRB method Growth inhibition of human SNB-19 cells measured after 24 to 72 hrs by SRB method	[PMID: 37163949]
SNB-19	IC₅₀	37 μM Compound: 1, TMZ	Chemosensitization of MGMT-deficient human SNB19 cells after 5 days by MTT assay Chemosensitization of MGMT-deficient human SNB19 cells after 5 days by MTT assay	[PMID: 23895620]
SNB-19	IC₅₀	69.87 μM Compound: TMZ	Cytotoxicity effect against human SNB-19 cells assessed as cell growth inhibition incubated for 48 hrs by trypan blue exclusion assay Cytotoxicity effect against human SNB-19 cells assessed as cell growth inhibition incubated for 48 hrs by trypan blue exclusion assay	[PMID: 34304559]
SNB-19	IC₅₀	> 250 μM Compound: 1, TMZ	Chemosensitization of human SNB19 cells expressing MGMT after 5 days by MTT assay Chemosensitization of human SNB19 cells expressing MGMT after 5 days by MTT assay	[PMID: 23895620]
T98G	GI₅₀	375 μM Compound: TMZ	Antiproliferative activity against human T98G cells assessed as cell growth inhibition incubated for 96 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human T98G cells assessed as cell growth inhibition incubated for 96 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 34731767]
T98G	IC₅₀	151 μM Compound: TMZ	Antiproliferative activity against human T98G cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human T98G cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37967166]
T98G	IC₅₀	5.7 x 10⁵ nM Compound: Temozolamide	Antiproliferative activity against human T98G cells after 5 days by MTT assay Antiproliferative activity against human T98G cells after 5 days by MTT assay	[PMID: 22608389]
T98G	IC₅₀	879 μM Compound: Temozolomide	Growth inhibition of human T98G cells after 72 hrs by MTT assay Growth inhibition of human T98G cells after 72 hrs by MTT assay	[PMID: 22809560]
TLX-5	IC₅₀	5 μM Compound: 1	In vitro cytotoxicity against mouse TLX5 lymphoma cells In vitro cytotoxicity against mouse TLX5 lymphoma cells	[PMID: 7739008]
U-251	EC₅₀	> 200 μM Compound: TMZ	Antiproliferative activity against human U251MG cells assessed as cell growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human U251MG cells assessed as cell growth inhibition measured after 72 hrs by SRB assay	[PMID: 31978780]
U-251	GI₅₀	> 100 μM Compound: Temozolomide	Growth inhibition of human U-251 cells measured after 24 to 72 hrs by SRB method Growth inhibition of human U-251 cells measured after 24 to 72 hrs by SRB method	[PMID: 37163949]
U-251	IC₅₀	12.74 μM Compound: TMZ	Cytotoxicity against human U-251MG cells assessed as decrease in cell viability incubated for 6 days by alamar blue assay Cytotoxicity against human U-251MG cells assessed as decrease in cell viability incubated for 6 days by alamar blue assay	[PMID: 34384944]
U-251	IC₅₀	189 μM Compound: TMZ	Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37967166]
U-251	IC₅₀	36.4 μM Compound: TMZ	Cytotoxicity against human U-251 cells by MTT assay Cytotoxicity against human U-251 cells by MTT assay	[PMID: 33915258]
U-251	IC₅₀	36.4 μM Compound: Temozolomide	Cytotoxicity against human U251 cells incubated for 24 hrs by MTT assay Cytotoxicity against human U251 cells incubated for 24 hrs by MTT assay	[PMID: 31891260]
U-251	IC₅₀	43.51 μM Compound: Temozolomide	Antiproliferative activity against human U-251MG cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human U-251MG cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38377560]
U-251	IC₅₀	455 μM Compound: TMZ	Cytotoxicity against human U251MG cells assessed as reduction in cell survival measured after 72 hrs by MTT assay Cytotoxicity against human U251MG cells assessed as reduction in cell survival measured after 72 hrs by MTT assay	[PMID: 30975504]
U-251	IC₅₀	6.426 μM Compound: TMZ	Cytotoxicity against cold atmospheric plasma (CAP)-treated human U-251MG cells assessed as decrease in cell viability treated with CAP for 30 secs followed by incubated with compound for 6 days by alamar blue assay Cytotoxicity against cold atmospheric plasma (CAP)-treated human U-251MG cells assessed as decrease in cell viability treated with CAP for 30 secs followed by incubated with compound for 6 days by alamar blue assay	[PMID: 34384944]
U-251	IC₅₀	7.284 μM Compound: TMZ	Cytotoxicity against cold atmospheric plasma (CAP)-treated human U-251MG cells assessed as decrease in cell viability treated with CAP for 15 secs followed by incubated with compound for 6 days by alamar blue assay Cytotoxicity against cold atmospheric plasma (CAP)-treated human U-251MG cells assessed as decrease in cell viability treated with CAP for 15 secs followed by incubated with compound for 6 days by alamar blue assay	[PMID: 34384944]
U-251	IC₅₀	> 100 μM Compound: TMZ	Antiproliferative activity against human U251 cells after 48 hrs by MTT assay Antiproliferative activity against human U251 cells after 48 hrs by MTT assay	[PMID: 26651221]
U-251	IC₅₀	> 200 μM Compound: TMZ	Inhibition of cell proliferation of human U251 cells assessed as cell viability after 72 hrs by sulforhodamine B assay Inhibition of cell proliferation of human U251 cells assessed as cell viability after 72 hrs by sulforhodamine B assay	[PMID: 25442304]
U-251	IC₅₀	> 250 μM Compound: 1, TMZ	Cytotoxicity against human U251 cells after 5 days by MTT assay Cytotoxicity against human U251 cells after 5 days by MTT assay	[PMID: 24900418]
U-251	IC₅₀	> 30 μM Compound: TMZ	Antiproliferative activity against human U-251 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against human U-251 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 34656900]
U-251	IC₅₀	> 50 μM Compound: TMZ	Antiproliferative activity against human U-251 cells assessed as cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human U-251 cells assessed as cell viability measured after 72 hrs by MTT assay	[PMID: 37385078]
U-251	IC₅₀	> 50 μM Compound: TMZ	Antiproliferative activity against human U-251 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human U-251 cells incubated for 48 hrs by MTT assay	[PMID: 38784471]
U-251	IC₅₀	> 500 μM Compound: TMZ	Anticancer activity against human U-251 cells assessed as cell growth inhibition inhibition incubated for 3 days Anticancer activity against human U-251 cells assessed as cell growth inhibition inhibition incubated for 3 days	[PMID: 37201660]
U-373MG ATCC	GI₅₀	369 μM Compound: 1; TMZ	Growth inhibition of MGMT-transfected human U373 cells expressing MGMT after 7 days by MTT assay Growth inhibition of MGMT-transfected human U373 cells expressing MGMT after 7 days by MTT assay	[PMID: 30108945]
U-373MG ATCC	GI₅₀	395 μM Compound: 1; TMZ	Growth inhibition of MGMT-transfected human U373 cells after 7 days by MTT assay Growth inhibition of MGMT-transfected human U373 cells after 7 days by MTT assay	10.1039/C6MD00384B
U-373MG ATCC	GI₅₀	68 μM Compound: 1; TMZ	Growth inhibition of vehicle-transfected human U373 cells after 7 days by MTT assay Growth inhibition of vehicle-transfected human U373 cells after 7 days by MTT assay	[PMID: 30108945]
U-373MG ATCC	GI₅₀	72.9 μM Compound: 1; TMZ	Growth inhibition of empty vector transfected human U373 cells after 7 days by MTT assay Growth inhibition of empty vector transfected human U373 cells after 7 days by MTT assay	10.1039/C6MD00384B
U-373MG ATCC	IC₅₀	220 μM Compound: Temozolomide	Growth inhibition of human U373 cells after 72 hrs by MTT assay Growth inhibition of human U373 cells after 72 hrs by MTT assay	[PMID: 22809560]
U-87MG ATCC	EC₅₀	> 200 μM Compound: TMZ	Antiproliferative activity against human U87MG cells assessed as cell growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human U87MG cells assessed as cell growth inhibition measured after 72 hrs by SRB assay	[PMID: 31978780]
U-87MG ATCC	IC₅₀	1.1 x 10⁶ nM Compound: Temozolomide	Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 48 hrs under hypoxia condition by MTT assay Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 48 hrs under hypoxia condition by MTT assay	[PMID: 32186874]
U-87MG ATCC	IC₅₀	113.36 μM Compound: Temozolomide	Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth incubated for 68 hrs by CCK-8 assay Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth incubated for 68 hrs by CCK-8 assay	[PMID: 39213937]
U-87MG ATCC	IC₅₀	19.38 μM Compound: Temozolomide	Cytotoxicity against human U87 cells assessed as growth inhibition after 72 hrs by SRB assay Cytotoxicity against human U87 cells assessed as growth inhibition after 72 hrs by SRB assay	10.1039/C4MD00264D
U-87MG ATCC	IC₅₀	203 μM Compound: TMZ	Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37967166]
U-87MG ATCC	IC₅₀	2898 μM Compound: TMZ	Cytotoxicity against human U-87 MG cells using best fit nonlinear regression analysis Cytotoxicity against human U-87 MG cells using best fit nonlinear regression analysis	[PMID: 35044783]
U-87MG ATCC	IC₅₀	3186 μM Compound: TMZ	Cytotoxicity against human U-87 MG cells assessed as cell viability using raw interpretation method Cytotoxicity against human U-87 MG cells assessed as cell viability using raw interpretation method	[PMID: 35044783]
U-87MG ATCC	IC₅₀	4.9 x 10⁴ nM Compound: Temozolamide	Antiproliferative activity against human U87 cells after 5 days by MTT assay Antiproliferative activity against human U87 cells after 5 days by MTT assay	[PMID: 22608389]
U-87MG ATCC	IC₅₀	6.4 x 10⁵ nM Compound: Temozolomide	Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 48 hrs under normoxia condition by MTT assay Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 48 hrs under normoxia condition by MTT assay	[PMID: 32186874]
U-87MG ATCC	IC₅₀	> 200 μM Compound: TMZ	Inhibition of cell proliferation of human U87MG cells assessed as cell viability after 72 hrs by sulforhodamine B assay Inhibition of cell proliferation of human U87MG cells assessed as cell viability after 72 hrs by sulforhodamine B assay	[PMID: 25442304]
U-87MG ATCC	IC₅₀	> 200 μM Compound: TMZ	Cytotoxicity against human U-87 MG cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Cytotoxicity against human U-87 MG cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 34534673]
U-87MG ATCC	IC₅₀	> 200 μM Compound: TMZ	Cytotoxicity against human U-87 MG cells incubated for 48 hrs by CCK8 assay Cytotoxicity against human U-87 MG cells incubated for 48 hrs by CCK8 assay	[PMID: 39136241]
U-87MG ATCC	IC₅₀	> 30 μM Compound: TMZ	Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 34656900]
U-87MG ATCC	IC₅₀	> 50 μM Compound: TMZ	Antiproliferative activity against human U87 cells assessed as cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human U87 cells assessed as cell viability measured after 72 hrs by MTT assay	[PMID: 37385078]
U-87MG ATCC	IC₅₀	> 50 μM Compound: Temozolomide	Cytotoxicity against human U87 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human U87 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29789258]
U138-MG	IC₅₀	26 μM Compound: Temozolomide	Cytotoxicity against human U138MG cells incubated for 48 hrs by MTT assay Cytotoxicity against human U138MG cells incubated for 48 hrs by MTT assay	[PMID: 23069682]
WM 266-4	IC₅₀	> 100 μM Compound: TMZ	Cytotoxicity against human WM 266-4 cells assessed as cell viability measured after 96 hrs by XTT assay Cytotoxicity against human WM 266-4 cells assessed as cell viability measured after 96 hrs by XTT assay	[PMID: 34507011]
WiDr	IC₅₀	1720 μM Compound: temozolomide	Cytotoxicity against human WiDr cells overexpressing MGMT after 48 hrs by trypan blue staining-based hemocytometric analysis Cytotoxicity against human WiDr cells overexpressing MGMT after 48 hrs by trypan blue staining-based hemocytometric analysis	[PMID: 25874335]
carcinoma cell line	IC₅₀	91 μM Compound: 1	Antitumor activity against human NCI ovarian carcinoma cell line panel Antitumor activity against human NCI ovarian carcinoma cell line panel	[PMID: 15615536]

体外研究
(In Vitro)

Temozolomide (TZM) 是一种甲基化剂，可穿过血脑屏障，适用于恶性神经胶质瘤和转移性黑色素瘤。Temozolomide 可有效对抗以低水平 O⁶-烷基鸟嘌呤 DNA 烷基转移酶 (OGAT) 和功能错配修复系统 (MR)^[1]为特征的肿瘤细胞。测定 Temozolomide (TZM) 在不同细胞系中的 IC₅₀ 值范围为 14.1 至 234.6 μM，分为两个明显不同的组：低 IC₅₀ 的细胞系值 (<50 μM)，包括 A172 (14.1±1.1 μM) 和 LN229 细胞 (14.5±1.1 μM)，以及具有高 IC₅₀ 值 (>100 μM) 的那些，包括 SF268 (147.2±2.1 μM) 和 SK-N-SH 细胞 (234.6±2.3 μM)^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

与对照相比，Temozolomide (TZM) 作为单一药物不会显著增加中值生存时间 (MST)。值得注意的是，在施用 100 或 200 mg/kg Temozolomide 之前，颅内注射 NU1025 可显著延长对照组或仅接受 Temozolomide 处理组的寿命。分割 Temozolomide 时，使用该方案获得的寿命延长 (ILS) 高于 NU1025 联合单次注射 Temozolomide 时观察到的 (生存曲线统计比较：NU1025 颅内注射 + Temozolomide 100 mg/kg×2 vs NU1025 + Temozolomide 200 mg/kg；P=0.023)^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

194.15

Formula

C₆H₆N₆O₂

CAS 号

85622-93-1

性状

固体

颜色

White to yellow

中文名称

替莫唑胺

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 20.83 mg/mL (107.29 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : 2.86 mg/mL (14.73 mM; 超声助溶)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	5.1507 mL	25.7533 mL	51.5066 mL
5 mM	1.0301 mL	5.1507 mL	10.3013 mL
10 mM	0.5151 mL	2.5753 mL	5.1507 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (6.44 mM); 澄清溶液

此方案可获得 ≥ 1.25 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (6.44 mM); 澄清溶液

此方案可获得 ≥ 1.25 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (6.44 mM); 澄清溶液

此方案可获得 ≥ 1.25 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： PBS
Solubility: 6.67 mg/mL (34.35 mM); 澄清溶液; 超声助溶 (<60°C)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.98%

选择批次：

Data Sheet (652 KB) SDS (585 KB)

COA (289 KB) RP-HPLC (136 KB) 元素分析报告 (213 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Tentori L, et al. Combined treatment with temozolomide and poly(ADP-ribose) polymerase inhibitor enhances survival of mice bearing hematologic malignancy at the central nervous system site. Blood. 2002 Mar 15;99(6):2241-4. [Content Brief]

[2]. Mathieu V, et al. Combining Anti-Human VEGF with temozolomide increases the antitumor efficacy of temozolomide in a human glioblastoma orthotopic xenograft model. Neoplasia. 2008 Dec;10(12):1383-92. [Content Brief]

[3]. Perazzoli G, et al. Temozolomide Resistance in Glioblastoma Cell Lines: Implication of MGMT, MMR, P-Glycoprotein and CD133 Expression. PLoS One. 2015 Oct 8;10(10):e0140131. [Content Brief]

Cell Assay ^[1]	The murine lymphoma cell line L5178Y of DBA/2 (H-2^d/H-2^d) origin is cultured in RPMI-1640 containing 10% fetal calf serum and antibiotics. Inhibition of PARP is obtained by treating cells (10⁵ cells/mL) with 8-hydroxy-2-methylquinazolin-4[³H]-1 (NU1025), at a concentration (25 μM) that abrogates PARP activity. Cells are then exposed to Temozolomide (7.5-125 μM) and are cultured for 3 days. Cell growth is evaluated by counting viable cells in quadruplicate, and apoptosis is assessed by flow cytometry analysis of DNA content. Long-term survival is analyzed by colony-formation assay^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] Male B6D2F1 (C57BL/6×DBA/2) mice are used. L5178Y cells (10⁴ in 0.03 mL RPMI-1640) are then injected intracranially, through the center-middle area of the frontal bone to a 2-mm depth, using a 0.1-mL glass microsyringe and a 27-gauge disposable needle. To evaluate tumor cell growth, brains are fixed in 10% phosphate-buffered formaldehyde, and histologic sections (5 μm) are cut along the axial plane, stained with hematoxylin-eosin, and analyzed by light microscopy. Temozolomide is dissolved in DMSO (40 mg/mL), diluted in saline (5 mg/mL), and administered intraperitoneally on day 2 after tumor injection at 100 mg/kg or 200 mg/kg, doses commonly used for in vivo preclinical studies. Because cytotoxicity induced by Temozolomide and PARP inhibitors can be improved by fractionated modality of treatment, in selected groups a total dose of 200 mg/kg Temozolomide is divided in 2 doses of 100 mg/kg given on days 2 and 3. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Tentori L, et al. Combined treatment with temozolomide and poly(ADP-ribose) polymerase inhibitor enhances survival of mice bearing hematologic malignancy at the central nervous system site. Blood. 2002 Mar 15;99(6):2241-4. [Content Brief] [2]. Mathieu V, et al. Combining Anti-Human VEGF with temozolomide increases the antitumor efficacy of temozolomide in a human glioblastoma orthotopic xenograft model. Neoplasia. 2008 Dec;10(12):1383-92. [Content Brief] [3]. Perazzoli G, et al. Temozolomide Resistance in Glioblastoma Cell Lines: Implication of MGMT, MMR, P-Glycoprotein and CD133 Expression. PLoS One. 2015 Oct 8;10(10):e0140131. [Content Brief]

Temozolomide 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	5.1507 mL	25.7533 mL	51.5066 mL	128.7664 mL
	5 mM	1.0301 mL	5.1507 mL	10.3013 mL	25.7533 mL
	10 mM	0.5151 mL	2.5753 mL	5.1507 mL	12.8766 mL
DMSO	15 mM	0.3434 mL	1.7169 mL	3.4338 mL	8.5844 mL
	20 mM	0.2575 mL	1.2877 mL	2.5753 mL	6.4383 mL
	25 mM	0.2060 mL	1.0301 mL	2.0603 mL	5.1507 mL
	30 mM	0.1717 mL	0.8584 mL	1.7169 mL	4.2922 mL
	40 mM	0.1288 mL	0.6438 mL	1.2877 mL	3.2192 mL
	50 mM	0.1030 mL	0.5151 mL	1.0301 mL	2.5753 mL
	60 mM	0.0858 mL	0.4292 mL	0.8584 mL	2.1461 mL
	80 mM	0.0644 mL	0.3219 mL	0.6438 mL	1.6096 mL
	100 mM	0.0515 mL	0.2575 mL	0.5151 mL	1.2877 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Temozolomide85622-93-1NSC 362856 CCRG 81045 TMZ替莫唑胺NSC362856NSC-362856CCRG81045CCRG 81045CCRG-81045DNA Alkylator/CrosslinkerAutophagyApoptosisInhibitorinhibitorinhibit

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Temozolomide (Synonyms: 替莫唑胺; NSC 362856; CCRG 81045; TMZ)

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Temozolomide (Synonyms: 替莫唑胺; NSC 362856; CCRG 81045; TMZ)

Customer Review

Other Forms of Temozolomide:

Temozolomide 相关抗体

MCE 顾客使用本产品发表的 163 篇科研文献

Temozolomide 相关产品

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生物活性

实验参考方法

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Temozolomide 相关抗体:

摩尔计算器

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