A dual inhibitor of KIT and PDGFRα mutant kinases (IC50s = 0.27 and 0.24 nM for KITD816V and PDGFRαD842V

BLU-285 – 1 mg

Brand:
Cayman
CAS:
1703793-34-3
Storage:
-20
UN-No:
Non-Hazardous - /

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).{40523} 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 = D814Y 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.  

 

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SKU: 22985 - 1 mg Category:

Description

A dual inhibitor of KIT and PDGFRα mutant kinases (IC50s = 0.27 and 0.24 nM for KITD816V and PDGFRαD842V, respectively); >150-fold selective for KITD816V and PDGFRαD842V over a kinase panel at a concentration of 3 μM; has activity against a panel of KIT and PDGFRα loop mutants identified in patients with GISTs (IC50s = D814Y mastocytoma allograft mouse model and a GIST patient-derived mouse xenograft model in a dose-dependent manner when administered at doses ranging from 0.3-30 mg/kg

Formal name: (αS)-(4-fluorophenyl)-α-methyl-2-[4-[6-(1-methyl-1H-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]-1-piperazinyl]-5-pyrimidinemethanamine

Synonyms:  Avapritinib

Molecular weight: 498.6

CAS: 1703793-34-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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