BLU-285

BLU-285

CAT N°: 22985
Price:

From 48.00 40.80

BLU-285 is a dual inhibitor of KIT receptor and platelet-derived growth factor receptor ? (PDGFR?) tyrosine kinases with activating loop mutations (IC50s = 0.27 and 0.24 nM for KITD816V and PDGFR?D842V, respectively).{40523} It is >150-fold selective for KITD816V and PDGFR?D842V over a kinase panel at a concentration of 3 ?M. BLU-285 also has activity against a panel of KIT and PDGFR? 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 PDGFR?-driven malignancies.

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