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首页-小分子抑制剂&激动剂-Tyrosine Kinase-FGFR-SOMCL-286
SOMCL-286

Chemical Structure : SOMCL-286

CAS No.: 2126751-06-0

SOMCL-286 (SOMCL286 )

货号: PC-26356Not For Human Use, Lab Use Only.

SOMCL-286 (Compound 25a) is a highly potent dual FGFR/VEGFR inhibitor with IC50 of 1.0 nM against FGFR1, shows nearly equally high potency against FGFR1, FGFR2 and VEGFR-2 with IC50 values of 1.0, 4.5 and 2.9 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

SOMCL-286 (Compound 25a) is a highly potent dual FGFR/VEGFR inhibitor with IC50 of 1.0 nM against FGFR1, shows nearly equally high potency against FGFR1, FGFR2 and VEGFR-2 with IC50 values of 1.0, 4.5 and 2.9 nM, respectively.
SOMCL-286 has <0.5 nM against the FGFR1-positive KG-1cancer cell.
SOMCL-286 inhibited the proliferation of BAF3/VEGFR2 cell lines with an IC50 less than 1.5 nM.
SOMCL-286 demonstrated greater antiproliferative effects in all these FGFR1-3 subtype-selective cell lines than AZD4547, including FGFR1-amplified H1581 cells, FGFR1-translocated KG1 cells, FGFR2-amplified SNU-16 cells, FGFR3-amplified RT112 cells and FGFR3-mutated UMUC14 cells.
SOMCL-286 suppressed tumor growth in a dose-dependent manner, with tumor growth inhibition rate (TGI) of 25.0% and 81.0% at doses of 10 mg/kg and 50 mg/kg (i.p.), respectively, in SNU-16 xenograft models.

物理化学性质&存储条件

分子量 495.58
分子式 C29H29N5O3
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

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

参考文献

1. Manman Wei, et al. Eur J Med Chem. 2018 Jun 25:154:9-28.

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