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Sorafenib tosylate

产品编号 T0093 CAS 475207-59-1

别名: 甲苯磺酸索拉非尼, Bay 43-9006

Sorafenib tosylate (Bay 43-9006) 是一种口服活性Raf 抑制剂，也是铁死亡激动剂。它是多激酶抑制剂，对VEGFR2，VEGFR3，PDGFRβ，FLT3和c-Kit 的IC50分别为 90 nM，15 nM，20 nM，57 nM 和 58 nM。它诱导细胞自噬和凋亡，有抗肿瘤活性。

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Sorafenib tosylate, CAS 475207-59-1

规格	价格/CNY	货期
5 mg	￥ 153	现货
10 mg	￥ 198	现货
25 mg	￥ 318	现货
50 mg	￥ 453	现货
100 mg	￥ 656	现货
200 mg	￥ 812	现货
500 mg	￥ 997	现货
1 g	￥ 1,470	现货
1 mL * 10 mM (in DMSO)	￥ 351	现货

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其他形式的 Sorafenib tosylate:

Sorafenib-d3
现货
Sorafenib
现货
Sorafenib-d4
询价

选择批次

纯度: 99.81%

纯度: 99.2%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).
靶点活性	c-Kit:68 nM (cell free), PDGFRβ:57 nM (cell free), B-Raf V599E:38 nM (cell free), Raf-1:6 nM (cell free0, B-Raf:22 nM (cell free), VEGFR3:20 nM (cell free)
体外活性	除 Raf-1 外，Sorafenib 还能在生化试验中抑制 VEGFR-3（IC50：20 nM）、BRAF wt（IC50：22 nM）、B-RAF V599E（IC50：38 nM）、VEGFR-2（IC50：90 nM）、PDGFR-β（IC50：57 nM）、c-KIT（IC50：68 nM）和 Flt3（IC50：58 nM）[1]。当 10-0505 细胞与抗人源抗 HGF 抗体共同处理时，Sorafenib 诱导的 c-Met、p70S6K 和 4EBP1 磷酸化显著降低，这表明Sorafenib 治疗会导致 HGF 分泌增加和c-Met 和 mTOR 靶点激活[2]。
体内活性	Sorafenib Tosylate（10、30、50及100 mg/kg，口服）依剂量依赖方式抑制06-0606及10-0505异种移植瘤生长（P<0.01）。Sorafenib同样显著降低了06-0606和10-0505异种移植瘤的生长速率。经Sorafenib（50/100 mg/kg）处理的小鼠中，06-0606瘤体重分别约为对照组的13%及5%。50 mg剂量的Sorafenib在带有5-1318、26-1004和10-0505细胞系的小鼠中显著抑制肿瘤生长（P<0.01）。在50 mg剂量下，06-0606、26-1004、5-1318和10-0505异种移植瘤中，Sorafenib和安慰剂处理瘤体末次治疗中位重量（mg）的T/C比分别是0.13、0.10、0.12和0.49 [2]。存活率在二乙基亚硝胺（DENA）组为73.3%，Sorafenib组为83.3%，相较之下正常对照组为100%。DENA组较正常对照组显著增加肝脏指数（增加1.51倍，p<0.05），而Sorafenib处理则与DENA组相比显著降低肝脏指数（p<0.05），Sorafenib组的肝脏指数显著降至低于正常对照组水平 [3]。
激酶实验	Recombinant baculoviruses expressing Raf-1 (residues 305–648) and B-Raf (residues 409–765) are purified as fusion proteins. Full-length human MEK-1 is generated by PCR and purified as a fusion protein from Escherichia coli lysates. Sorafenib tosylate is added to a mixture of Raf-1 (80 ng), or B-Raf (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. Human VEGFR2 (KDR) kinase domain is expressed and purified from Sf9 lysates. Time-resolved fluorescence energy transfer assays for VEGFR2 are performed in 96-well opaque plates in the time-resolved fluorescence energy transfer format. Final reaction conditions are as follows: 1 to 10 μM ATP, 25 nM poly GT-biotin, 2 nM Europium-labeled phospho (p)-Tyr antibody (PY20), 10 nM APC, 1 to 7 nM cytoplasmic kinase domain in final concentrations of 1% DMSO, 50 mM HEPES (pH 7.5), 10 mM MgCl2, 0.1 mM EDTA, 0.015% Brij-35, 0.1 mg/mL BSA, and 0.1% β-mercaptoethanol. Reaction volumes are 100 μL and are initiated by the addition of enzyme. Plates are read at both 615 and 665 nM on a Perkin-Elmer VictorV Multilabel counter at ~1.5 to 2.0 hours after reaction initiation. Signal is calculated as a ratio: (665 nm/615 nM) × 10,000 for each well. For IC50 generation, Sorafenib tosylate is added before the enzyme initiation. A 50-fold stock plate is made with Sorafenib tosylate serially diluted 1:3 in a 50% DMSO/50% distilled water solution. Final Sorafenib tosylate concentrations range from 10 μM to 4.56 nM in 1% DMSO.
细胞实验	Tumor cell lines were plated at 2 × 105 cells per well in 12-well tissue culture plates in DMEM growth media (10% heat-inactivated FCS) overnight. Cells were washed once with serum-free media and incubated in DMEM supplemented with 0.1% fatty acid-free BSA containing various concentrations of BAY 43-9006 in 0.1% DMSO for 120 minutes to measure changes in basal pMEK 1/2, pERK 1/2, or pPKB. Cells were washed with cold PBS (PBS containing 0.1 mmol/L vanadate) and lysed in a 1% (v/v) Triton X-100 solution containing protease inhibitors. Lysates were clarified by centrifugation, subjected to SDS-PAGE, transferred to nitrocellulose membranes, blocked in TBS-BSA, and probed with anti-pMEK 1/2 (Ser217/Ser221; 1:1000), anti-MEK 1/2, anti-pERK 1/2 (Thr202/Tyr204; 1:1000), anti-ERK 1/2, anti-pPKB (Ser473; 1:1000), or anti-PKB primary antibodies. Blots were developed with horseradish peroxidase (HRP)-conjugated secondary antibodies and developed with Amersham ECL reagent on Amersham Hyperfilm [1].
动物实验	Female NCr-nu/nu mice (Taconic Farms, Germantown, NY) were used for all studies. Three to five million cells were injected s.c. into the right flank of each mouse. DLD-1 tumors were established and maintained as a serial in vivo passage of s.c. fragments (3 × 3 mm) implanted in the flank using a 12-gauge trocar. A new generation of the passage was initiated every three weeks, and studies were conducted between generations 3 and 12 of this line. Treatment was initiated when tumors in all mice in each experiment ranged in size from 75 to 144 mg for antitumor efficacy studies and from 100 to 250 mg for studies of microvessel density and ERK phosphorylation. All treatment was administered orally once daily for the duration indicated in each experiment.

别名	甲苯磺酸索拉非尼, Bay 43-9006
分子量	637.03
分子式	C21H16ClF3N4O3·C7H8O3S
CAS No.	475207-59-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (78.49 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	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	0.314 mL	1.5698 mL	3.1396 mL	7.8489 mL
	10 mM	0.157 mL	0.7849 mL	1.5698 mL	3.9245 mL
	20 mM	0.0785 mL	0.3924 mL	0.7849 mL	1.9622 mL
	50 mM	0.0314 mL	0.157 mL	0.314 mL	0.7849 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

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. 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. 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.

文献引用

1. Gao X, Jiang P, Wei X, et al.Novel fusion protein PK5-RL-Gal-3C inhibits hepatocellular carcinoma via anti-angiogenesis and cytotoxicity.BMC cancer.2023, 23(1): 1-16.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Sorafenib tosylate 475207-59-1 Angiogenesis Apoptosis Autophagy MAPK Tyrosine Kinase/Adaptors Raf VEGFR FLT Ferroptosis PDGFR c-Kit inhibit CD135 Sorafenib FLT3 Raf kinases Sorafenib Tosylate Cluster of differentiation antigen 135 Inhibitor 甲苯磺酸索拉非尼 Vascular endothelial growth factor receptor Bay 43-9006 Fms like tyrosine kinase 3 inhibitor

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Sorafenib tosylate

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

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剂量换算

体内实验配液计算器

技术支持

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