S49076

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Chemical Structure| 1265965-22-7 同义名 : -
CAS号 : 1265965-22-7
货号 : A300808
分子式 : C22H22N4O4S
纯度 : 98%
分子量 : 438.5
MDL号 : MFCD28963943
存储条件：

Pure form Inert atmosphere,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(68.42 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • FGFR2

    FGFR2, IC50:17 nM

  • FGFR3

    FGFR3, IC50:15 nM

  • FGFR1

    FGFR1, IC50:18 nM
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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.28mL

0.46mL

0.23mL

11.40mL

2.28mL

1.14mL

22.81mL

4.56mL

2.28mL
参考文献

[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.