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Association details:
| Biomarker: | KIT V560G |
|---|---|
| Cancer: | Chronic Myeloid Leukemia |
| Drug: | dasatinib (c-KIT inhibitor, Bcr-abl tyrosine kinase inhibitor, Src kinase inhibitor, EphA2 receptor antagonist, PDGFR β antagonist) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis
Excerpt:
In contrast, dasatinib suppresses the growth of HMC-1.1V560G+, D816V- cells in the low nanomolar range and is approximately 5 times more potent than imatinib in this assay…Furthermore, dasatinib retains activity against HMC-1.2V560G+, D816V+ cells, although higher concentrations are required (Figure 2B). Dasatinib also shows a strong growth inhibitory activity against the P815 rodent mastocytoma line, which carries KITD814V, the murine equivalent of KIT D816V.
DOI:
https://doi.org/10.1182/blood-2005-10-3969
