Chemical Structure : FGFR2-FGFR4 inhibitor F-30
CAS No.:
2619509-67-8
FGFR2-FGFR4 inhibitor F-30
(FGFR2/4 inhibitor)
货号: PC-28537Not For Human Use, Lab Use Only.
FGFR2-FGFR4 inhibitor F-30 is a potent, selective covalent inhibitor of FGFR2/4 with IC50 of 7.8 nM and 11 nM for FGFR2 and FGFR4 respectively.
大包装，大折扣！
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
FGFR2-FGFR4 inhibitor F-30 is a potent, selective covalent inhibitor of FGFR2/4 with IC50 of 7.8 nM and 11 nM for FGFR2 and FGFR4 respectively.
F-30 shows much weaker activity against FGFR1 and FGFR3 with IC50 of 315 nM and 91 nM respectively.
F-30 exhibits a KI value of 4.6 nM for FGFR2, which was approximately 12-fold lower than that for FGFR1 (53 nM).
F-30 strongly suppresses the proliferation of Ba/F3 cells driven by FGFR2 or FGFR4, with IC50 values of 5.9 nM and 19 nM, respectively, with substantially reduced in FGFR1- and FGFR3-driven models (IC50=456 nM and 76 nM).
Cys477 is critical for the potent covalent inhibition of FGFR4 by F-30, and F-30 shows covalent binding to FGFR2 at Cys491.
F-30 retains potent activity against multiple clinically relevant FGFR2 mutations N549K/H/D, E565A, K641R, potently inhibits all tested mutant variants with IC50 values in the low nanomolar range.
F-30 is less effective against gatekeeper mutations.
F-30 inhibits the proliferation of FGFR-driven cancer cell lines and suppresses FGFR-mediated signaling pathways.
物理化学性质&存储条件
|
分子量
|
464.91
|
|
分子式
|
C24H21ClN4O4
|
|
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
|
3-(2-chloroacetamido)-N-(6-(3,5-dimethoxyphenyl)-1H-indazol-3-yl)benzamide
|
参考文献
1. Zhang L, et al. Biochem Pharmacol. 2026 Oct 20:118560.
