BLU-285
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- Product name: BLU-285
- CAS: 1703793-34-3
- MF: C26H27FN10
- MW: 498.56
- EINECS:-0
- MDL Number:MFCD31544325
- Synonyms:BLU-285;CPD1212;(1S)-1-(4-Fluorophenyl)-1-(2-{4-[6-(1-methyl-1H-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]-1-piperazinyl}-5-pyrimidinyl)ethanamine;Avapritinib(BLU-285);BLU-285 (Avapritinib);BLU-285;BLU 285;BLU285;CS-2474;BLU-N
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Properties
Density :1.42±0.1 g/cm3(Predicted)
storage temp. :Store at -20°C
solubility :DMSO:83.11(Max Conc. mg/mL);166.7(Max Conc. mM)
form :A crystalline solid
pka :6.96±0.10(Predicted)
color :White to light yellow
CAS DataBase Reference :1703793-34-3
storage temp. :Store at -20°C
solubility :DMSO:83.11(Max Conc. mg/mL);166.7(Max Conc. mM)
form :A crystalline solid
pka :6.96±0.10(Predicted)
color :White to light yellow
CAS DataBase Reference :1703793-34-3
Safety Information
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Description
BLU-285 is a dual inhibitor of KIT receptor and platelet-derived growth factor receptor α (PDGFRα) tyrosine kinases with activating loop mutations (IC50s = 0.27 and 0.24 nM for KITD816V and PDGFRαD842V, respectively). It is >150-fold selective for KITD816V and PDGFRαD842V over a kinase panel at a concentration of 3 μM. BLU-285 also has activity against a panel of KIT and PDGFRα loop mutants identified in patients with gastrointestinal stromal tumors (GISTs; IC50s = <100 nM). It inhibits growth of cancer cell lines containing wild-type and mutant KIT and PDGFRα, demonstrating increased potency in cell lines expressing KIT and PDGFRα with activating loop mutations. BLU-285 (0.3-30 mg/kg) reduces tumor volume in a P815 KITD814Y mastocytoma allograft mouse model and a GIST patient-derived mouse xenograft model in a dose-dependent manner. Formulations containing BLU-285 have been used to treat KIT- and PDGFRα-driven malignancies.More related product prices
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