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首页-小分子抑制剂&激动剂-Tyrosine Kinase-FLT3-FYJ-195
FYJ-195

Chemical Structure : FYJ-195

CAS No.:

FYJ-195 (FYJ195)

货号: PC-26900Not For Human Use, Lab Use Only.

FYJ-195 is a highly potent type II FLT3 inhibitor with IC50 of 2.03 nM for FLT3-ITD, overcomes recalcitrant gatekeeper F691L and activation loop D835V/Y variants.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

FYJ-195 is a highly potent type II FLT3 inhibitor with IC50 of 2.03 nM for FLT3-ITD, overcomes recalcitrant gatekeeper F691L and activation loop D835V/Y variants.
FYJ-195 exhibited single-digit nanomolar potency against Ba/F3-FLT3-ITD-F691L (IC50 = 9.09 nM) and subnanomolar activity against Ba/F3-FLT3-ITD-D835Y (IC50 = 4.64 nM) and Ba/F3-FLT3-ITD-D835V (IC50 = 0.76 nM).
FYJ-195 induced profound tumor regression (TGI = 125%) in the MV4-11 xenograft model (10 mg/kg) and achieved robust tumor growth suppression (TGI = 68.6%) in the Ba/F3-FLT3-ITD-F691L model (50 mg/kg).
FYJ-195 effectively blocked FLT3 signaling and induced apoptosis without observable toxicity.

物理化学性质&存储条件

分子量 525.54
分子式 C26H26F3N7O2
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

1-(4-(3-aminoisoxazolo[5,4-b]pyridin-4-yl)phenyl)-3-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)urea

参考文献

1. Yang J, et al. J Med Chem. 2026 May 23. doi: 10.1021/acs.jmedchem.6c00648.

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