Sorafenib tosylate (Synonyms: 甲苯磺酸索拉非尼; Bay 43-9006 tosylate)

目录号: HY-10201A 纯度: 99.98%: Data Sheet SDS COA 产品使用指南
FAQs
技术支持

Sorafenib tosylate (Bay 43-9006 tosylate) 是一种有效的口服活性 Raf 抑制剂，对 Raf-1 和 B-Raf 的 IC₅₀ 分别为 6 nM 和 20 nM。Sorafenib tosylate 是一种多激酶抑制剂，对 VEGFR2，VEGFR3，PDGFRβ，FLT3 和 c-Kit 的 IC₅₀ 分别为 90 nM，15 nM，20 nM，57 nM 和 58 nM。Sorafenib tosylate 诱导细胞自噬 (autophagy) 和凋亡 (apoptosis)，并具有抗肿瘤活性。Sorafenib tosylate 也是一种 ferroptosis 激动剂。

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Sorafenib tosylate Chemical Structure

CAS No. : 475207-59-1

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥500	In-stock
1 mg	￥140	In-stock
5 mg	￥281	In-stock
10 mg	￥450	In-stock
50 mg	￥650	In-stock
100 mg	￥850	In-stock
500 mg	￥1200	In-stock
1 g		询价
5 g		询价

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Customer Review

Other Forms of Sorafenib tosylate:

MCE 顾客使用本产品发表的 260 篇科研文献

RT-PCR

Cell Viability Assay

Proliferation Assay

: Sorafenib tosylate purchased from MCE. Usage Cited in: Nat Commun. 2025 Jan 2;16(1):87. [Abstract]; The cell viability of YAP-, YAP-S127A-, or YAP-R124F-overexpressed Huh-7 cells cultured in methionine-deprived medium (MD) and treated with sorafenib (1.5-3 μM) for 24 h.

: Sorafenib tosylate purchased from MCE. Usage Cited in: ACS Nano. 2023 Nov 28;17(22):22240-22258. [Abstract]; Western blot to detect the ferritin H protein level by the gain or loss of URB1-AS1 in sorafenib-sensitive or sorafenib-resistant HepG2 cells.

: Sorafenib tosylate purchased from MCE. Usage Cited in: ACS Nano. 2023 Nov 28;17(22):22240-22258. [Abstract]; qPCR showing the nuclear and cytoplasmic fractions of URB1-AS1 in sorafenib-resistant HepG2 cells with β-actin and MALAT1 as cytoplasmic and nuclear controls, respectively.

: Sorafenib tosylate purchased from MCE. Usage Cited in: Acta Pharm Sin B. 2023 Jun;13(6):2645-2662.; HeLa and SiHa cells were treated with condition medium (CM) from human PBMC-derived M0 macrophages (Ctrl) and TAM. And then cells were treated with indicated dose of Sorafenib (Sora) for 48 h. Inhibition ratio of cell viability was detected by CCK-8 assay.

: Sorafenib tosylate purchased from MCE. Usage Cited in: Acta Pharm Sin B. 2023 Oct;13(10):4253-4272. [Abstract]; Sorafenib (12.5-125 μM; 24 h) inhibits the viability of PANC-1 cells in a dose-dependent manner.

: Sorafenib tosylate purchased from MCE. Usage Cited in: Acta Pharm Sin B. 2023 Oct;13(10):4253-4272. [Abstract]; PANC-1 cells were transfected with the recombinant plasmid for 24 h and treated with sorafenib (0–70 μmol/L) for another 24 h, and then total cellular extracts were subjected to Western blotting using antibodies against caspase-3, GSDME and β-tubulin.

: Sorafenib tosylate purchased from MCE. Usage Cited in: Discov Oncol. 2023 May 27;14(1):83. [Abstract]; Sorafenib (3 µM; 24 h) significantly inhibits the cell proliferation of HepG2 and Hep3B.

: Sorafenib tosylate purchased from MCE. Usage Cited in: Discov Oncol. 2023 May 27;14(1):83. [Abstract]; Sorafenib (0.25, 0.5, 1, 2, 4, 6 µM; 24 h) significantly inhibits the cell viability of HepG2 and Hep3B.

: Sorafenib tosylate purchased from MCE. Usage Cited in: Int J Biol Sci. 2018 Apr 25;14(5):577-585. [Abstract]; Hep3B, HepG2 and Huh7 cells are treated with 5 μM Sorafenib. The expressing levels of JAK1, JAK2, STAT3, SHP1, SHP2, actin and phosphorylation levels of STAT3 are determined by western blot using the antibodies, respectively.

: Sorafenib tosylate purchased from MCE. Usage Cited in: Oncol Rep. 2018 Sep;40(3):1525-1532. [Abstract]; SMMC-7721 and HepG2 cells are treated with 4 µM Sorafenib and 100 µM Berberine alone or in combination (4 µM Sorafenib+100 µM Berberine) for 72 h, and the expression levels of apoptosis-associated proteins are measured by western blot analysis.

: Sorafenib tosylate purchased from MCE. Usage Cited in: Br J Cancer. 2017 Sep 26;117(7):974-983. [Abstract]; The effect of the AKT inhibitor MK2206 (10 μM) on the expression levels of phosphor-AKT, AKT, and STMN1 in TKI-pretreated NCI-H460 cells. β-actin is used as a loading control.

: Sorafenib tosylate purchased from MCE. Usage Cited in: J Pharmacol Exp Ther. 2017 Aug;362(2):219-229. [Abstract]; The combination of sorafenib and CAI induces apoptosis in NSCLC. Effect of 10 μM CAI and/or 5 μM Sorafenib on the expression of cleaved PARP and cleaved caspase-. Protein levels of cleaved PARP and cleaved caspase-3 from treated cell lysates are normalized against GAPDH levels.

: Sorafenib tosylate purchased from MCE. Usage Cited in: Am J Cancer Res. 2017 Dec 1;7(12):2503-2514. [Abstract]; VPA potentiates anti-tumor effects of Sorafenib tosylate in vivo. The expression of cleaved caspase9, cleaved caspase3, cleaved PARP from tumor tissue homogenates are analyzed by western blot.

: Sorafenib tosylate purchased from MCE. Usage Cited in: Endocr J. 2017 Nov 29;64(11):1115-1123. [Abstract]; Effect of Sorafenib on phosphorylation of ERK and AKT. Thyroid cancer cells are treated for 30 minutes with 10 μM Sorafenib, 10 μM Forskolin, and combination therapy of 10 μM Sorafenib with 10 μM Forskolin. The levels of ERK and AKT phosphorylation are examined by immunoblot analysis. β-actin is used as the control. Sorafenib suppresses phosphorylation of ERK, but not of AKT.

: Sorafenib tosylate purchased from MCE. Usage Cited in: Endocr J. 2017 Nov 29;64(11):1115-1123. [Abstract]; Effect of Sorafenib and Forskolin on expression of CDK4 and CDK regulatory proteins. Thyroid cancer cells are treated for 24 hours with 10 μM Sorafenib, 10 μM Forskolin, and combination therapy of 10 μM Sorafenib with 10 μM Forskolin. The expression of cyclin D1, CDK4, and phosphorylation of RB are examined by immunoblot analysis. β-actin is used as the control. The combination therapy suppresses expression of cyclin D1, and Forskolin monotherapy suppresses expression of cyclin D1 in TPC-1 and W

: Sorafenib tosylate purchased from MCE. Usage Cited in: Oncotarget. 2017 May 2;8(18):29771-29784. [Abstract]; Sorafenib inhibits Pin1 biosynthesis and accumulation in Huh7 and HepG2 cells. Cells are treated with 5 or 10 μM Sorafenib for indicated times. Pin1 protein expression is determined by Western Blot.

: Sorafenib tosylate purchased from MCE. Usage Cited in: Int J Clin Exp Pathol. 2015 Apr 1;8(4):3871-81. [Abstract]; The relationship between SOX9 and Raf/MEK/ERK signaling pathway. Co-treatment of si-SOX9-1 and Sorafenib (10uM, 15uM)/SU 11248 (2 uM, 3 uM) significantly decreases expression of MEK1 and its phosphorylated protein (p-MEK1/2, p-ERK1/2) as assayed by Western blot (with GAPDH as internal control).

: Sorafenib tosylate purchased from MCE. Usage Cited in: Int J Clin Exp Pathol. 2015 Apr 1;8(4):3871-81. [Abstract]; The relationship between SOX9 and Raf/MEK/ERK signaling pathway. Co-treatment of si-SOX9-1 and Sorafenib (10uM, 15uM)/SU 11248 (2 uM, 3 uM) significantly decreases expression of MEK1 and its phosphorylated protein (p-MEK1/2, p-ERK1/2) as assayed by RT-PCR (with β-actin as internal control).

Sorafenib tosylate 相关产品

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Sorafenib tosylate (Bay 43-9006 tosylate) is a potent and orally active Raf inhibitor with IC₅₀s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib tosylate is a multikinase inhibitor with IC₅₀s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib tosylate induces autophagy and apoptosis. Sorafenib tosylate has anti-tumor activity. Sorafenib tosylate is a ferroptosis activator^[1].

IC₅₀ & Target^[1]

VEGFR3

20 nM (IC₅₀)

Braf

22 nM (IC₅₀)

Raf-1

6 nM (IC₅₀)

VEGFR2

90 nM (IC₅₀)

Braf^V599E

38 nM (IC₅₀)

PDGFRβ

57 nM (IC₅₀)

c-Kit

68 nM (IC₅₀)

Flt3

58 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
Caco-2	CC₅₀	1.17 μM Compound: SORAFENIB	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay	10.21203/rs.3.rs-23951/v1
Caco-2	IC₅₀	1.55 μM Compound: SORAFENIB	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging	10.21203/rs.3.rs-23951/v1
CAKI-1	GI₅₀	3.2 μM Compound: NSC 747971	Antiproliferative activity against human CAKI-1 cells after 48 hrs by SRB assay Antiproliferative activity against human CAKI-1 cells after 48 hrs by SRB assay	[PMID: 22560627]
EKVX	GI₅₀	2.5 μM Compound: NSC 747971	Antiproliferative activity against human EKVX cells after 48 hrs by SRB assay Antiproliferative activity against human EKVX cells after 48 hrs by SRB assay	[PMID: 22560627]
HeLa	EC₅₀	> 10 μM Compound: Nexavar	Toxicity in human HeLa cells assessed as cell cycle arrest at G2M phase by flow cytometry based phenotypic drug discovery based assay Toxicity in human HeLa cells assessed as cell cycle arrest at G2M phase by flow cytometry based phenotypic drug discovery based assay	[PMID: 22409666]
Hep 3B2	IC₅₀	1.5 μM Compound: 6	Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by SRB assay Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by SRB assay	[PMID: 30108693]
HepG2	IC₅₀	214.8 nM Compound: ST	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33002846]
HT-29	GI₅₀	2.5 μM Compound: NSC 747971	Antiproliferative activity against human HT-29 cells after 48 hrs by SRB assay Antiproliferative activity against human HT-29 cells after 48 hrs by SRB assay	[PMID: 22560627]
Huh-7	IC₅₀	1.6 μM Compound: 6	Cytotoxicity against human HuH7 cells assessed as growth inhibition after 72 hrs by SRB assay Cytotoxicity against human HuH7 cells assessed as growth inhibition after 72 hrs by SRB assay	[PMID: 30108693]
HUVEC	IC₅₀	1954 nM Compound: ST	Antiproliferative activity against human HUVEC assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human HUVEC assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33002846]
Mahlavu	IC₅₀	0.7 μM Compound: 6	Cytotoxicity against human Mahlavu cells assessed as growth inhibition after 72 hrs by SRB assay Cytotoxicity against human Mahlavu cells assessed as growth inhibition after 72 hrs by SRB assay	[PMID: 30108693]
MCF7	IC₅₀	1384 nM Compound: ST	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33002846]
MCF7	GI₅₀	2.5 μM Compound: NSC 747971	Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay	[PMID: 22560627]
MDA-MB-231	IC₅₀	349.3 nM Compound: ST	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33002846]
MDA-MB-435	GI₅₀	2 μM Compound: NSC 747971	Antiproliferative activity against human MDA-MB-435 cells after 48 hrs by SRB assay Antiproliferative activity against human MDA-MB-435 cells after 48 hrs by SRB assay	[PMID: 22560627]
OVCAR-3	GI₅₀	3.2 μM Compound: NSC 747971	Antiproliferative activity against human OVCAR3 cells after 48 hrs by SRB assay Antiproliferative activity against human OVCAR3 cells after 48 hrs by SRB assay	[PMID: 22560627]
Sf9	IC₅₀	12.5 nM Compound: Nexavar	Inhibition of GST-tagged recombinant human VEGFR2 expressed in Sf9 cells by radiometric assay Inhibition of GST-tagged recombinant human VEGFR2 expressed in Sf9 cells by radiometric assay	[PMID: 24368209]
SNB-19	GI₅₀	3.2 μM Compound: NSC 747971	Antiproliferative activity against human SNB19 cells after 48 hrs by SRB assay Antiproliferative activity against human SNB19 cells after 48 hrs by SRB assay	[PMID: 22560627]
SW-620	GI₅₀	3.2 μM Compound: NSC 747971	Antiproliferative activity against human SW620 cells after 48 hrs by SRB assay Antiproliferative activity against human SW620 cells after 48 hrs by SRB assay	[PMID: 22560627]
TK-10	GI₅₀	5 μM Compound: NSC 747971	Antiproliferative activity against human TK10 cells after 48 hrs by SRB assay Antiproliferative activity against human TK10 cells after 48 hrs by SRB assay	[PMID: 22560627]
UACC-257	GI₅₀	2 μM Compound: NSC 747971	Antiproliferative activity against human UACC257 cells after 48 hrs by SRB assay Antiproliferative activity against human UACC257 cells after 48 hrs by SRB assay	[PMID: 22560627]

体外研究
(In Vitro)

Sorafenib tosylate 还在生化测定中抑制 BRAF^wt (IC₅₀=22 nM)、BRAF^V599E (IC₅₀=38 nM)、VEGFR-2 (IC₅₀=90 nM)、VEGFR-3 (IC₅₀=20 nM)、PDGFR-β (IC₅₀=57 nM)、c-KIT (IC₅₀=68 nM) 和 Flt3 (IC₅₀=58 nM)^[1]。
当 10-0505 细胞与抗人抗 HGF 抗体共同处理时，Sorafenib tosylate 诱导的 c-Met、p70S6K 和 4EBP1 磷酸化显著降低，这表明用 Sorafenib tosylate 处理会导致 HGF 分泌增加以及 c-Met 和 mTOR 靶标的激活^[2]。

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

体内研究
(In Vivo)

Sorafenib tosylate (10、30、50 和 100 mg/kg，口服) 以剂量依赖性方式抑制 06-0606 和 10-0505 异种移植瘤的肿瘤生长(P<0.01) 。Sorafenib 还显著降低了 06-0606 和 10-0505 异种移植瘤的生长速度。在用 50 mg/kg 和 100 mg/kg Sorafenib 治疗的小鼠中，06-0606 肿瘤的重量分别约为对照组的 13% 和 5%。50 mg/kg 剂量的 Sorafenib 显著抑制 5-1318、26-1004 和 10-0505 系小鼠的肿瘤生长 (P<0.01) 。对于 50 mg/kg 的剂量，06-0606、26-1004、5-1318 和 10-0505 异种移植瘤的 T/C 比率 (其中 T 和 C 分别是治疗结束时 Sorafenib 和载体治疗的肿瘤的中位重量 (mg)) 分别为 0.13、0.10、0.12 和 0.49^[2]。
二乙基亚硝胺 (DENA) 组存活率为 73.3 %，Sorafenib 组存活率为 83.3 %，而正常对照组存活率为 100 %。与正常对照组相比，DENA 组的肝脏指数显著增加 (增加 1.51 倍，p<0.05)，而与 DENA 组相比，Sorafenib 治疗组的肝脏指数显著降低 (p<0.05)。Sorafenib 组的肝指数显著降低至低于正常对照组的肝指数^[3]。

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

Clinical Trial

分子量

637.03

Formula

C₂₈H₂₄ClF₃N₄O₆S

CAS 号

475207-59-1

性状

固体

颜色

White to off-white

中文名称

甲苯磺酸索拉非尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 100 mg/mL (156.98 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5698 mL	7.8489 mL	15.6978 mL
5 mM	0.3140 mL	1.5698 mL	3.1396 mL
10 mM	0.1570 mL	0.7849 mL	1.5698 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, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C储存时，请在1年内使用， -20°C储存时，请在6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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.92 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.92 mM); 澄清溶液

此方案可获得 ≥ 2.5 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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, 1 year; -20°C, 6 months (sealed storage, away from moisture)

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 (647 KB) SDS (393 KB)

COA (282 KB) HNMR (306 KB) RP-HPLC (243 KB) MS (69 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Wilhelm SM, et al. BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res. 2004 Oct 1;64(19):7099-109. [Content Brief]

[2]. Huynh H, et al. Sorafenib and rapamycin induce growth suppression in mouse models of hepatocellular carcinoma. J Cell Mol Med. 2009 Aug;13(8B):2673-83. [Content Brief]

[3]. El-Ashmawy NE, et al. Sorafenib effect on liver neoplastic changes in rats: more than a kinase inhibitor. Clin Exp Med. 2016 Apr 16. [Content Brief]

[4]. Zhu W, et al. Combination of sorafenib and Valproic acid synergistically induces cell apoptosis and inhibits hepatocellular carcinoma growth via down-regulating Notch3 and pAkt. Am J Cancer Res. 2017 Dec 1;7(12):2503-2514. [Content Brief]

Kinase Assay ^[1]	To test compound inhibition against various RAF kinase isoforms, Sorafenib is added to a mixture of Raf-1 (80 ng), wt BRAF, or V599E BRAF (80 ng) with MEK-1 (1 μg) in assay buffer [20 mM Tris (pH 8.2), 100 mM NaCl, 5 mM MgCl₂, and 0.15% β-mercaptoethanol] at a final concentration of 1% DMSO. The RAF kinase assay (final volume of 50 μL) is initiated by adding 25 μL of 10 μM γ-[³³P]ATP (400 Ci/mol) and incubated at 32°C for 25 minutes. Phosphorylated MEK-1 is harvested by filtration onto a phosphocellulose mat, and 1% phosphoric acid is used to wash away unbound radioactivity. After drying by microwave heating, a β-plate counter is used to quantify filter-bound radioactivity^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[2]	The 10-0505, 06-0606, and 26-1004 tumors are finely minced and washed three times with modified Eagle medium (MEM). Cells are harvested by centrifuging at 800× g for 10 min. Cells are treated with 3 or 6 μM of Sorafenib in serum free MEM in the presence or absence of 5 μg/mL anti-human hepatocyte growth factor (HGF) antibody for 48 hrs. A total of 2 mL of conditioned medium from vehicle- or Sorafenib-treated (without anti-human antibody) is collected and concentrated using a VIVASPIN 20 and secreted HGF in conditioned medium is determined by western blotting^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]^[3]	Mice^[2] For dose-response experiment, mice bearing the 06-0606 and 10-0505 xenografts are given four doses of Sorafenib (10, 30, 50 and 100 mg/kg daily) orally for 12 days. Each treatment group comprised of five mice. To investigate the antitumor effects of Sorafenib, mice bearing tumors are orally administered 50 mg/kg Sorafenib daily for 12 days. Each treatment group is comprised of 14 animals and each experiment is repeated at least twice. Treatment started on day 7 after tumor implantation. By this time, the HCC xenografts reached the size of approximately 100 mm³. To study the effects of Rapamycin plus Sorafenib on the growth of 10-0505 xenograft, mice bearing tumors (14 per group) are orally administered either 200 μL of vehicle, or 50 mg/kg of Sorafenib, or 1 mg/kg of Rapamycin, or Rapamycin plus Sorafenib daily for indicated days. Tumor growth is monitored at least twice weekly by Vernier caliper measurement of the length and width of tumor. Tumor volume is calculated as follows: [length×width²×π/6]. At the end of the study, the mice are killed with body and tumor weights being recorded, and the tumors harvested for analysis. Rats^[3] In the study, 100- to 120-g male albino rats are utilized. After acclimatization period, rats are weighed and randomly divided into three groups: Group 1 (normal control group; n=10) is given the vehicle daily for 8 weeks. Group 2 (DENA group; n=15) receive i.p. single dose of 200 mg/kg DENA. Group 3 (Sorafenib group; n=12) is given Sorafenib orally at a dose of 10 mg/kg daily for 2 weeks, 6 weeks after DENA i.p. injection. At the end of the experiment (8 weeks), rats are weighed, anesthetized by ether, and killed, and their livers are dissected. Fresh liver is washed twice with ice-cold saline, dried on clean paper towel, and weighed. Liver index is calculated as liver weight (g)/final body weight (g)×100. The liver is divided into five portions: one portion is preserved in 10 % formalin for histopathological examination and the other portions are immediately frozen in liquid nitrogen and stored at −80°C. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Wilhelm SM, et al. BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res. 2004 Oct 1;64(19):7099-109. [Content Brief] [2]. Huynh H, et al. Sorafenib and rapamycin induce growth suppression in mouse models of hepatocellular carcinoma. J Cell Mol Med. 2009 Aug;13(8B):2673-83. [Content Brief] [3]. El-Ashmawy NE, et al. Sorafenib effect on liver neoplastic changes in rats: more than a kinase inhibitor. Clin Exp Med. 2016 Apr 16. [Content Brief] [4]. Zhu W, et al. Combination of sorafenib and Valproic acid synergistically induces cell apoptosis and inhibits hepatocellular carcinoma growth via down-regulating Notch3 and pAkt. Am J Cancer Res. 2017 Dec 1;7(12):2503-2514. [Content Brief]

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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

DMSO	1 mM	1.5698 mL	7.8489 mL	15.6978 mL	39.2446 mL
	5 mM	0.3140 mL	1.5698 mL	3.1396 mL	7.8489 mL
	10 mM	0.1570 mL	0.7849 mL	1.5698 mL	3.9245 mL
	15 mM	0.1047 mL	0.5233 mL	1.0465 mL	2.6163 mL
	20 mM	0.0785 mL	0.3924 mL	0.7849 mL	1.9622 mL
	25 mM	0.0628 mL	0.3140 mL	0.6279 mL	1.5698 mL
	30 mM	0.0523 mL	0.2616 mL	0.5233 mL	1.3082 mL
	40 mM	0.0392 mL	0.1962 mL	0.3924 mL	0.9811 mL
	50 mM	0.0314 mL	0.1570 mL	0.3140 mL	0.7849 mL
	60 mM	0.0262 mL	0.1308 mL	0.2616 mL	0.6541 mL
	80 mM	0.0196 mL	0.0981 mL	0.1962 mL	0.4906 mL
	100 mM	0.0157 mL	0.0785 mL	0.1570 mL	0.3924 mL

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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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Sorafenib tosylate (Synonyms: 甲苯磺酸索拉非尼; Bay 43-9006 tosylate)

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