Monomethyl auristatin E (Synonyms: MMAE; SGD-1010; Vedotin)

目录号: HY-15162G: Data Sheet SDS 产品使用指南
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Monomethyl auristatin E (MMAE) (GMP) 是 GMP 级别的 Monomethyl auristatin E (HY-15162)。Monomethyl auristatin E 是一种微管蛋白聚合抑制剂。

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Monomethyl auristatin E Chemical Structure

CAS No. : 474645-27-7

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生物活性
纯度 & 产品资料
参考文献

生物活性

Monomethyl auristatin E (MMAE) (GMP) is Monomethyl auristatin E (HY-15162) produced by using GMP guidelines. Monomethyl auristatin E is a tubulin polymerization inhibitor^[1].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	EC₅₀	0.0005 μM Compound: Monomethyl auristatin E	Antiproliferative activity against human A549 cells after 72 hrs by MTS assay Antiproliferative activity against human A549 cells after 72 hrs by MTS assay	[PMID: 28972755]
A549	IC₅₀	0.59 nM Compound: MMAE	Antiproliferative activity against human A549 cells after 4 days by XTT assay Antiproliferative activity against human A549 cells after 4 days by XTT assay	[PMID: 23845743]
A549	IC₅₀	1.3 nM Compound: 2; MMAE	Cytotoxicity against human A549 cells after 2 days by cell titer 96 aqueous one solution based assay Cytotoxicity against human A549 cells after 2 days by cell titer 96 aqueous one solution based assay	[PMID: 29454703]
BT-474	GI₅₀	0.22 nM Compound: 4, MMAE	Cytotoxicity against human BT474 cells assessed as cell viability incubated fore 4 days by MTS assay Cytotoxicity against human BT474 cells assessed as cell viability incubated fore 4 days by MTS assay	[PMID: 25431858]
BXPC-3	GI₅₀	> 1.39 nM Compound: 2b	Growth inhibition of human BxPC3 cells incubated for 48 hrs by MTT assay Growth inhibition of human BxPC3 cells incubated for 48 hrs by MTT assay	[PMID: 28211277]
BXPC-3	GI₅₀	> 1.39 nM Compound: Desmethylauristatin E	Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay	[PMID: 28895394]
BXPC-3	GI₅₀	> 1.39 nM Compound: Desmethylauristatin E	Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay	[PMID: 28926240]
CWR22R	CC₅₀	1.44 nM Compound: MMAE	Cytotoxicity against human 22Rv1 cells expressing PMSA measured using MTT assay Cytotoxicity against human 22Rv1 cells expressing PMSA measured using MTT assay	[PMID: 34797052]
DU-145	GI₅₀	0.418 nM Compound: 2b	Growth inhibition of human DU145 cells incubated for 48 hrs by MTT assay Growth inhibition of human DU145 cells incubated for 48 hrs by MTT assay	[PMID: 28211277]
DU-145	GI₅₀	0.418 nM Compound: Desmethylauristatin E	Growth inhibition of human DU145 cells after 48 hrs by SRB assay Growth inhibition of human DU145 cells after 48 hrs by SRB assay	[PMID: 28895394]
DU-145	GI₅₀	0.418 nM Compound: Desmethylauristatin E	Growth inhibition of human DU145 cells after 48 hrs by SRB assay Growth inhibition of human DU145 cells after 48 hrs by SRB assay	[PMID: 28926240]
DU-145	IC₅₀	0.55 nM Compound: MMAE	Cytotoxicity against human DU-145 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay Cytotoxicity against human DU-145 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay	[PMID: 36327103]
DU-145	IC₅₀	0.62 nM Compound: MMAE	Cytotoxicity against human DU-145 cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay Cytotoxicity against human DU-145 cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay	[PMID: 36327103]
H3396	IC₅₀	0.1 nM Compound: 3; MMAE	Cytotoxicity against human H3396 cells assessed as inhibition of cell growth incubated for 96 hrs by Alamar blue assay Cytotoxicity against human H3396 cells assessed as inhibition of cell growth incubated for 96 hrs by Alamar blue assay	[PMID: 39068862]
HEK-293T	IC₅₀	0.068 nM Compound: MMAE	Cytotoxicity against HEK293T cells assessed as inhibition in cell growth Cytotoxicity against HEK293T cells assessed as inhibition in cell growth	[PMID: 33974423]
HGC-27	IC₅₀	7.18 nM Compound: MMAE	Cytotoxicity against KK-LC-1-negative human HGC-27 cells incubated for 72 hrs by CCK-8 assay Cytotoxicity against KK-LC-1-negative human HGC-27 cells incubated for 72 hrs by CCK-8 assay	[PMID: 35932567]
HeLa	IC₅₀	1 nM Compound: MMAE	Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay	[PMID: 36327103]
HeLa	IC₅₀	1.1 nM Compound: MMAE	Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay	[PMID: 36327103]
KB	IC₅₀	0.19 nM Compound: MMAE	Antiproliferative activity against human KB cells after 4 days by XTT assay Antiproliferative activity against human KB cells after 4 days by XTT assay	[PMID: 23845743]
KM-20L2	GI₅₀	0.599 nM Compound: 2b	Growth inhibition of human KM20L2 cells incubated for 48 hrs by MTT assay Growth inhibition of human KM20L2 cells incubated for 48 hrs by MTT assay	[PMID: 28211277]
KM-20L2	GI₅₀	0.599 nM Compound: Desmethylauristatin E	Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay	[PMID: 28895394]
KM-20L2	GI₅₀	0.599 nM Compound: Desmethylauristatin E	Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay	[PMID: 28926240]
L1210	IC₅₀	2.1 nM Compound: 2; MMAE	Cytotoxicity against mouse L1210 cells after 2 days by cell titer 96 aqueous one solution based assay Cytotoxicity against mouse L1210 cells after 2 days by cell titer 96 aqueous one solution based assay	[PMID: 29454703]
LNCaP	IC₅₀	0.71 nM Compound: MMAE	Cytotoxicity against human LNCaP cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay Cytotoxicity against human LNCaP cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay	[PMID: 36327103]
LNCaP	IC₅₀	0.79 nM Compound: MMAE	Cytotoxicity against human LNCaP cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay Cytotoxicity against human LNCaP cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay	[PMID: 36327103]
MCF7	GI₅₀	0.404 nM Compound: 2b	Growth inhibition of human MCF7 cells incubated for 48 hrs by MTT assay Growth inhibition of human MCF7 cells incubated for 48 hrs by MTT assay	[PMID: 28211277]
MCF7	GI₅₀	0.404 nM Compound: Desmethylauristatin E	Growth inhibition of human MCF7 cells after 48 hrs by SRB assay Growth inhibition of human MCF7 cells after 48 hrs by SRB assay	[PMID: 28895394]
MCF7	GI₅₀	0.404 nM Compound: Desmethylauristatin E	Growth inhibition of human MCF7 cells after 48 hrs by SRB assay Growth inhibition of human MCF7 cells after 48 hrs by SRB assay	[PMID: 28926240]
MDA-MB-231	IC₅₀	0.25 nM Compound: MMAE	Antiproliferative activity against human MDA-MB-231 cells after 4 days by XTT assay Antiproliferative activity against human MDA-MB-231 cells after 4 days by XTT assay	[PMID: 23845743]
MDA-MB-361	GI₅₀	0.49 nM Compound: 4, MMAE	Cytotoxicity against human MDA-MB-361 cells assessed as cell viability incubated fore 4 days by MTS assay Cytotoxicity against human MDA-MB-361 cells assessed as cell viability incubated fore 4 days by MTS assay	[PMID: 25431858]
MES-SA	IC₅₀	0.096 nM Compound: MMAE	Cytotoxicity against human MES-SA cells assessed as inhibition in cell growth Cytotoxicity against human MES-SA cells assessed as inhibition in cell growth	[PMID: 33974423]
MES-SA/Dx5	IC₅₀	88.19 nM Compound: MMAE	Cytotoxicity against human MES-SA/Dx5 cells assessed as inhibition in cell growth Cytotoxicity against human MES-SA/Dx5 cells assessed as inhibition in cell growth	[PMID: 33974423]
MKN-45	IC₅₀	10.7 nM Compound: MMAE	Cytotoxicity against KK-LC-1-positive human MKN-45 cells incubated for 72 hrs by CCK-8 assay Cytotoxicity against KK-LC-1-positive human MKN-45 cells incubated for 72 hrs by CCK-8 assay	[PMID: 35932567]
NCI-H460	GI₅₀	0.683 nM Compound: 2b	Growth inhibition of human NCI-H460 cells incubated for 48 hrs by MTT assay Growth inhibition of human NCI-H460 cells incubated for 48 hrs by MTT assay	[PMID: 28211277]
NCI-H460	GI₅₀	0.683 nM Compound: Desmethylauristatin E	Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay	[PMID: 28895394]
NCI-H460	GI₅₀	0.683 nM Compound: Desmethylauristatin E	Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay	[PMID: 28926240]
NCI-H524	IC₅₀	3.7 nM Compound: MMAE	Cytotoxicity in human NCI-H524 cells pre-incubated for 2 hrs followed by compound wash out and subsequently incubated for 70 hrs by Cell Titer Glo assay Cytotoxicity in human NCI-H524 cells pre-incubated for 2 hrs followed by compound wash out and subsequently incubated for 70 hrs by Cell Titer Glo assay	[PMID: 30735385]
NCI-N87	GI₅₀	0.54 nM Compound: 4, MMAE	Cytotoxicity against human NCI-N87 cells assessed as cell viability incubated fore 4 days by MTS assay Cytotoxicity against human NCI-N87 cells assessed as cell viability incubated fore 4 days by MTS assay	[PMID: 25431858]
NUGC-4	IC₅₀	10.97 nM Compound: MMAE	Cytotoxicity against KK-LC-1-positive human NUGC-4 cells incubated for 72 hrs by CCK-8 assay Cytotoxicity against KK-LC-1-positive human NUGC-4 cells incubated for 72 hrs by CCK-8 assay	[PMID: 35932567]
PC-3	CC₅₀	0.97 nM Compound: MMAE	Cytotoxicity against human PC-3 cells not expressing PMSA measured using MTT assay Cytotoxicity against human PC-3 cells not expressing PMSA measured using MTT assay	[PMID: 34797052]
SF-268	GI₅₀	0.432 nM Compound: 2b	Growth inhibition of human SF268 cells incubated for 48 hrs by MTT assay Growth inhibition of human SF268 cells incubated for 48 hrs by MTT assay	[PMID: 28211277]
SF-268	GI₅₀	0.432 nM Compound: Desmethylauristatin E	Growth inhibition of human SF268 cells after 48 hrs by SRB assay Growth inhibition of human SF268 cells after 48 hrs by SRB assay	[PMID: 28895394]
SF-268	GI₅₀	0.432 nM Compound: Desmethylauristatin E	Growth inhibition of human SF268 cells after 48 hrs by SRB assay Growth inhibition of human SF268 cells after 48 hrs by SRB assay	[PMID: 28926240]
SK-OV-3	IC₅₀	0.66 nM Compound: 2; MMAE	Cytotoxicity against human SKOV3 cells after 2 days by cell titer 96 aqueous one solution based assay Cytotoxicity against human SKOV3 cells after 2 days by cell titer 96 aqueous one solution based assay	[PMID: 29454703]
U-87MG ATCC	EC₅₀	0.0002 μM Compound: Monomethyl auristatin E	Antiproliferative activity against human U87 cells after 72 hrs by MTS assay Antiproliferative activity against human U87 cells after 72 hrs by MTS assay	[PMID: 28972755]

体外研究
(In Vitro)

Monomethyl auristatin E (MMAE) 在 CD30+ 在癌细胞内从 SGN-35 有效释放，并且由于其膜渗透性，能够对周围细胞发挥细胞毒活性^[1]。
Monomethyl auristatin E (MMAE) 以与有丝分裂停滞相关的时间表和剂量依赖性的方式使结直肠癌细胞和胰腺癌细胞对 IR 敏感。放射增敏作用表现为受照射细胞中克隆形成存活率下降和 DNA 双链断裂增加^[2]。

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

体内研究
(In Vivo)

Monomethyl auristatin E (MMAE) 与 IR 结合导致肿瘤生长延迟，肿瘤靶向 ACPP-cRGD-MMAE 与 IR 在异种移植模型中产生更稳健并显著延长的肿瘤消退^[2]。

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

Clinical Trial

分子量

717.98

Formula

C₃₉H₆₇N₅O₇

CAS 号

474645-27-7

性状

固体

颜色

Off-white to light yellow

运输条件

Shipping with dry ice.

储存方式

-20°C, protect from light

溶解性数据

细胞实验：

Ethanol 中的溶解度 : 50 mg/mL (69.64 mM; 超声加热助溶)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.3928 mL	6.9640 mL	13.9280 mL
5 mM	0.2786 mL	1.3928 mL	2.7856 mL
10 mM	0.1393 mL	0.6964 mL	1.3928 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。-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。

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

计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

Data Sheet (607 KB) SDS (644 KB) 产品使用指南 (1538 KB)

参考文献

[1]. Okeley, et al. Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate. Clinical Cancer Research (2010), 16(3), 888-897. [Content Brief]

[2]. Lisa Buckel, et al. Tumor radiosensitization by monomethyl auristatin E: mechanism of action and targeted delivery. Cancer Res. 2015 Apr 1;75(7):1376-87. [Content Brief]

Monomethyl auristatin E 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

Ethanol	1 mM	1.3928 mL	6.9640 mL	13.9280 mL	34.8199 mL
	5 mM	0.2786 mL	1.3928 mL	2.7856 mL	6.9640 mL
	10 mM	0.1393 mL	0.6964 mL	1.3928 mL	3.4820 mL
	15 mM	0.0929 mL	0.4643 mL	0.9285 mL	2.3213 mL
	20 mM	0.0696 mL	0.3482 mL	0.6964 mL	1.7410 mL
	25 mM	0.0557 mL	0.2786 mL	0.5571 mL	1.3928 mL
	30 mM	0.0464 mL	0.2321 mL	0.4643 mL	1.1607 mL
	40 mM	0.0348 mL	0.1741 mL	0.3482 mL	0.8705 mL
	50 mM	0.0279 mL	0.1393 mL	0.2786 mL	0.6964 mL
	60 mM	0.0232 mL	0.1161 mL	0.2321 mL	0.5803 mL

Help & FAQs

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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.

Keywords:

Monomethyl auristatin E (GMP)474645-27-7MMAE (GMP)SGD-1010 (GMP)Vedotin (GMP)Microtubule/TubulinADC PayloadApoptosisADC CytotoxinGMPADCauxiliary reagentMMAEcancerInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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Monomethyl auristatin E (Synonyms: MMAE; SGD-1010; Vedotin)

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Monomethyl auristatin E (Synonyms: MMAE; SGD-1010; Vedotin)

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