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首页-小分子抑制剂&激动剂-Tyrosine Kinase-FGFR-INCB126503
INCB126503

Chemical Structure : INCB126503

CAS No.: 2640089-88-7

INCB126503 (INCB-126503)

货号: PC-24894Not For Human Use, Lab Use Only.

INCB126503 is a highly potent, selective, orally bioavailable FGFR2/3 inhibitor with IC50 of 2.1/1.2 nM respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

INCB126503 is a highly potent, selective, orally bioavailable FGFR2/3 inhibitor with IC50 of 2.1/1.2 nM respectively.
INCB126503 shows potent activity when tested against both of the FGFR3 gatekeeper mutants FGFR3-V555L (IC50 = 0.92 nM) and FGFR3-V555 M (IC50 = 0.85 nM).
INCB126503 displays single-digit nanomolar potency against FGFR3 in BAF3 cells (IC50 = 6.8 nM) while featuring excellent selectivity over FGFR1 (58-fold), also is highly selective over FGFR4 (IC50 = 64 nM).
INCB126503 inhibits both pFGFR3 and pERK signaling in RT112/84 tumor cells following a single oral dose of 100 mg/kg in RT112/84 tumors, demonstrates significant antitumor efficacy without inducing hyperphosphatemia.

物理化学性质&存储条件

分子量 470.58
分子式 C27H30N6O2
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

Pyrrolo[1,2-a]pyrazin-7-ol, 2-[5-[5-(2,3-dimethylphenyl)-6-methoxy-1H-pyrazolo[4,3-b]pyridin-3-yl]-2-pyridinyl]octahydro-, (7R,8aS)-

参考文献

1. Nguyen MH, et al. ACS Med Chem Lett. 2025 May 17;16(6):1182-1189.

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