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首页-小分子抑制剂&激动剂-Tyrosine Kinase-FGFR-SOMCL-085
SOMCL-085

Chemical Structure : SOMCL-085

CAS No.: 2126751-12-8

SOMCL-085 (SOMCL085)

货号: PC-26355Not For Human Use, Lab Use Only.

SOMCL-085 is a potent multi-targeted FGFR inhibitor with IC50 of 1.8, 1.9 and 6.9 nM for FGFR1-3, simultaneously inhibits VEGFR and PDGFR.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

SOMCL-085 is a potent multi-targeted FGFR inhibitor with IC50 of 1.8, 1.9 and 6.9 nM for FGFR1-3, simultaneously inhibits VEGFR and PDGFR.
SOMCL-085 displays weaker activity against FGFR4 (IC50=319.9 nM).
SOMCL-085 significantly inhibits VEGFR1, VEGFR2, PDGFR-α, and PDGFR-β kinase activity, with potency that was equal or lower than that observed against FGFR1–3.
SOMCL-085 potently inhibits FGFR signaling, regardless of the mechanistic complexity of FGFR activation.
SOMCL-085 elicits significant effects against FGFR1–3-driven cancer cell proliferation via G1/S cell cycle arrest
SOMCL-085 (25 mg/kg and 50 mg/kg) significantly inhibits FGFR-mediated tumor growth in vivo, with tumor growth inhibition rates of 62.9% and 81.3% in FGFR2-amplified gastric cancer cell line SNU16 xenograft mouse models.

物理化学性质&存储条件

分子量 525.61
分子式 C30H31N5O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-((2-(4-(4-(2-hydroxyethyl)piperazin-1-yl)benzamido)pyridin-4-yl)oxy)-N-methyl-1-naphthamide

参考文献

1. Xi-Fei Jiang, et al. Acta Pharmacol Sin. 2018 Feb;39(2):243-250.

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