Chemical Structure : FYJ-195
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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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.
| 分子量 | 525.54 | |
| 分子式 | C26H26F3N7O2 | |
| 外观性状 | Solid | |
| 储存条件 |
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| Solubility |
10 mM in DMSO |
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1. Yang J, et al. J Med Chem. 2026 May 23. doi: 10.1021/acs.jmedchem.6c00648.
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