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Association details:
| Biomarker: | BCR-ABL1 Q252R |
|---|---|
| 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:
Overriding Imatinib Resistance with a Novel ABL Kinase Inhibitor
Excerpt:
BMS-354825 is an orally bioavailable ABL kinase inhibitor with two-log increased potency relative to imatinib that retains activity against 14 of 15 imatinib-resistant BCR-ABL mutants. BMS354825 prolongs survival of mice with BCR-ABL– driven disease and inhibits proliferation of BCR-ABL–positive bone marrow progenitor cells from patients with imatinib-sensitive and imatinib-resistant CML....In vitro analysis of cell-growth inhibition of imatinib-resistant Ba/F3 cells expressing the indicated BCR-ABL mutants. Viable cell counts were performed in triplicate after 48 hours of exposure to BMS-354825 and normalized to the dimethyl sulfoxide–treated sample.
DOI:
10.1126/science.1099480
