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CAS No.: 848318-25-2

SSR128129E Catalog No. CSN15810

Synonyms: SSR

SSR128129E is an allosteric modulator of FGFR by binding to the extracellular FGFR domain.

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技术信息

生物活性

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].
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

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
- 2.8876 mL
- 14.4378 mL
- 28.8757 mL
- 5 mM
- 0.5775 mL
- 2.8876 mL
- 5.7751 mL
- 10 mM
- 0.2888 mL
- 1.4438 mL
- 2.8876 mL

技术信息

CAS号

848318-25-2

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H15N2NaO4

运输

蓝冰

分子量

346.31

别名

SSR

溶解度

DMSO	70.0 mg/mL (202.1 mM)
Water	50.0 mg/mL (144.4 mM) warming

动物实验配方

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