Chemical Structure : FYJ-195
CAS No.:
FYJ-195
(FYJ195)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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525.54
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Formula
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C26H26F3N7O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1-(4-(3-aminoisoxazolo[5,4-b]pyridin-4-yl)phenyl)-3-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)urea
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References
1. Yang J, et al. J Med Chem. 2026 May 23. doi: 10.1021/acs.jmedchem.6c00648.
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