BLU-654 | KIT V654A inhibitor | Probechem Biochemicals

Chemical Structure : BLU-654

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BLU-654 (BLU654)

货号: PC-26312Not For Human Use, Lab Use Only.

BLU-654 is a potent, selective inhibitor of mutant KIT V654A with IC50 of 5.7 nM for mutant KIT autophosphorylation (pKIT 11/13) inhibition, 15-fold selective over WT KIT.

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生物&药学活性

BLU-654 is a potent, selective inhibitor of mutant KIT V654A with IC50 of 5.7 nM for mutant KIT autophosphorylation (pKIT 11/13) inhibition, 15-fold selective over WT KIT.
BLU-654 has a substantial selectivity margin over PDGFRβ (219-fold) and exhibited a favorable kinome selectivity profile with an S(10) of 0.06.
BLU-654 elicits a dose and time-dependent pSTAT5 reduction with a free in vivo IC50 of 4.2 nM at 4 h in PK/PD study using a cell-derived xenograft (CDX) model in HMC1.1 11/13 cell line.
BLU-654 (3, 10, 30, and 60 mg/kg once daily by oral gavage) showed strong antitumor activity in the 11/13 CDX model.

物理化学性质&存储条件

分子量	429.50
分子式	C21H28FN7O2
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	(S)-1-(4-(6-((6-Amino-2-(1-fluoroethyl)pyrimidin-4-yl)amino)-4-isopropoxypyridin-3-yl)-1H-pyrazol-1-yl)-2-methylpropan-2-ol

参考文献

1. Moine L, et al. J Med Chem. 2026 Mar 10. doi: 10.1021/acs.jmedchem.5c03554.

BLU-654 (BLU654)

生物&药学活性

物理化学性质&存储条件

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BLU-654 (BLU654)

生物&药学活性

物理化学性质&存储条件

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