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CAS No.: 1265965-22-7

S49076 Catalog No. CSN19153

Synonyms: S49076

S49076 is a potent inhibitor of MET, AXL/MER, and FGFRs.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述S49076 is a novel and potent inhibitor of MET/MET mutations, AXL/MER, and FGFR1/2/3 with IC50 values of 1nM/1-17nM, 7nM/2nM, 18nM/17nM/15nM, respectively. S49076 potently blocked cellular phosphorylation of MET (3-10nM), AXL (10-1000nM), and FGFRs (>300nM) and inhibited downstream signaling p-FRS2 and p-ERK in vitro. S49076 inhibited viability (IC50 values were 3, 167, and >10μM for GTL-16, SNU-16, and MKN-7, respectively), motility (IC50 for inhibition of HGF-induced cell motility of 14nM in A549 cells), and three-dimensional colony formation of cancer cells expressing MET, AXL, or FGFRs. Orally administered S49076 at doses ranging in 0.78-12.5mg/kg inhibited MET signaling in subcutaneous xenografts in balb/c nu/nu mice at doses, suggesting its good pharmacodynamics. Oral administration of S49076 inhibited tumor growth in mice xenograft GTL-16, U87-MG and SNU-16 at doses ranging in 3.125-50mg/kg, 6.25-50mg/kg and 37.5-100mg/kg, respectively^[2].
作用机制S49076 can bind to MET ATP-pocket.^[2]
动物研究
剂量
Mice: 0.78 mg/kg - 50 mg/kg^[1] (p.o.)

给药途径
p.o.
参考文献

动物研究
剂量	Mice: 0.78 mg/kg - 50 mg/kg^[1] (p.o.)
给药途径	p.o.

[1] Burbridge MF, Bossard CJ, et al. S49076 is a novel kinase inhibitor of MET, AXL, and FGFR with strong preclinical activity alone and in association with bevacizumab. Mol Cancer Ther. 2013 Sep;12(9):1749-62.
[2] Burbridge MF, Bossard CJ, Saunier C, Fejes I, Bruno A, Léonce S, Ferry G, Da Violante G, Bouzom F, Cattan V, Jacquet-Bescond A, Comoglio PM, Lockhart BP, Boutin JA, Cordi A, Ortuno JC, Pierré A, Hickman JA, Cruzalegui FH, Depil S. S49076 is a novel kinase inhibitor of MET, AXL, and FGFR with strong preclinical activity alone and in association with bevacizumab. Mol Cancer Ther. 2013 Sep;12(9):1749-62. doi: 10.1158/1535-7163.MCT-13-0075. Epub 2013 Jun 26. PMID: 23804704.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2805 mL
- 11.4025 mL
- 22.8050 mL
- 5 mM
- 0.4561 mL
- 2.2805 mL
- 4.5610 mL
- 10 mM
- 0.2281 mL
- 1.1403 mL
- 2.2805 mL

技术信息

CAS号

1265965-22-7

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H22N4O4S

运输

蓝冰

分子量

438.50

别名

S49076

溶解度

DMSO	80.0 mg/mL (182.4 mM)
Water	insoluble

动物实验配方

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