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Association details:
| Biomarker: | FLT3 D835A |
|---|---|
| Cancer: | Acute Myelogenous Leukemia |
| Drug: | tandutinib (MLN518) (c-KIT inhibitor, PDGFR inhibitor, FLT3 inhibitor) |
| Direction: | Resistant |
Evidence:
Source:
Title:
Variable sensitivity of FLT3 activation loop mutations to the small molecule tyrosine kinase inhibitor MLN518
Excerpt:
Each FLT3 activation loop mutant, including D835Y, D835A, D835E, D835H, D835N, D835V, D835del, and I836del, transformed Ba/F3 cells…MLN518 inhibited FLT3 autophosphorylation and phosphorylation of STAT5 and ERK in FLT3-ITD-transformed Ba/F3 cells with an IC(50) (50% inhibition of cell viability) of approximately 500 nM...Thus, certain activation loop mutations in FLT3 simultaneously confer resistance to small molecule inhibitors.
DOI:
10.1182/blood-2003-12-4446
