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Association details:
| Biomarker: | FLT3 D835H |
|---|---|
| Cancer: | Acute Myelogenous Leukemia |
| Drug: | sunitinib (c-KIT inhibitor, VEGFR inhibitor, PDGFR inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
Emergence of polyclonal FLT3 tyrosine kinase domain mutations during sequential therapy with sorafenib and sunitinib in FLT3-ITD-positive acute myeloid leukemia
Excerpt:
Sunitinib suppressed leukemic clones with D835H and F691L mutations, but not D835Y. Cells expressing sorafenib-resistant FLT3 mutations were sensitive to sunitinib in vitro.
DOI:
https://dx.doi.org/10.1158%2F1078-0432.CCR-13-1323
Source:
Title:
SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo
Excerpt:
These results suggest that further exploration of SU11248 activity in AML patients is warranted....SU11248 inhibited phosphorylation of FLT3-ITD with an IC50 of less than 10 nM. Similarly, phosphorylation of activation loop mutants Asp835Tyr, Asp835Val, and Asp835His was inhibited by SU11248, with IC50 values of 30 to 300 nM (Figure 2)....SU11248 also inhibited phosphorylation of Asp835 point mutations, Asp835Val, Asp835His, and Asp835Tyr.
DOI:
10.1182/blood-2002-07-2307
