SSR128129E

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Chemical Structure| 848318-25-2 同义名 : SSR
CAS号 : 848318-25-2
货号 : A349538
分子式 : C18H15N2NaO4
纯度 : 99%+
分子量 : 346.312
MDL号 : MFCD25976751
存储条件：

Pure form Keep in dark place,Inert atmosphere,Room temperature

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

DMSO: 55 mg/mL(158.82 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

  • FGFR1

    FGFR1, IC50:1.9 μM
描述 The FGFR (fibroblast growth factors receptor) superfamily with its 18 ligands and four receptors has been implicated in cancer, inflammation, and the escape of tumor vascularization from VEGF (vascular endothelial growth factor) inhibitor treatment. SSR128129E is a multi-FGFR signaling inhibitor with an IC50 value of 1.9 μM for FGFR1. In human umbilical venous endothelial cells (HUVECs) expressing FGFR1, SSR128129E inhibited FGF2-induced EC (endothelial cell) proliferation (IC50: 31 ± 1.6 nM), migration (IC50: 15.2 ± 4.5 nM), and lamellipodia formation in a dose dependent manner. In arthritic mice, oral administration of SSR128129E (30 mg/kg/day) reduced the number of limbs affected by redness, swelling, and deformity. Moreover, SSR128129E and αVEGFR2 each inhibited Panc02 tumor growth by 40%, while the combination treatment inhibited tumor growth by 70%[3].
作用机制 SSR128129E binds to the extracellular FGFR domain[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.89mL

0.58mL

0.29mL

14.44mL

2.89mL

1.44mL

28.88mL

5.78mL

2.89mL
参考文献

[1]Bono F, De Smet F, et al. Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties. Cancer Cell. 2013 Apr 15;23(4):477-88.

[2]Dol-Gleizes F, Delesque-Touchard N, et al. A new synthetic FGF receptor antagonist inhibits arteriosclerosis in a mouse vein graft model and atherosclerosis in apolipoprotein E-deficient mice. PLoS One. 2013 Nov 4;8(11):e80027.

[3]Bono F, De Smet F, Herbert C, et al. Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties. Cancer Cell. 2013;23(4):477-488