Chemical Structure : BLU-654
CAS No.:
2999638-62-7
BLU-654
(BLU654)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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429.50
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Formula
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C21H28FN7O2
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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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(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
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References
1. Moine L, et al. J Med Chem. 2026 Mar 10. doi: 10.1021/acs.jmedchem.5c03554.
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