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KW2449
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CAS No. | 1000669-72-6 | Cat. No. | BCP02848 |
Name | KW2449 | ||
Synonyms | KW 2449;KW-2449; | ||
SMILES | |||
Chemical Name | |||
Formula | C20H20N4O | M. Wt | 332.4 |
Purity | 98% | Storage | Store at 4-8°C |
Description | KW-2449, a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase, is under investigation to treat leukemia patients. KW-2449 shows the potent growth inhibitory effects on leukemia cells with FLT3 mutations by inhibition of the FLT3 kinase, resulting in the down-regulation of phosphorylated-FLT3/STAT5, G1 arrest, and apoptosis. Oral administration of KW-2449 shows dose-dependent and significant tumor growth inhibition in FLT3-mutated xenograft model with minimum bone marrow suppression. In FLT3 wild-type human leukemia, KW-2449 induces the reduction of phosphorylated histone H3, G2/M arrest, and apoptosis. In Imatinib-resistant leukemia, KW-2449 contributes to release of the resistance by the simultaneous down-regulation of BCR/ABL and Aurora kinases. The inhibitory activity of KW-2449 is not affected by the presence of human plasma protein, such as α1-acid glycoprotein. KW-2449 has potent growth inhibitory activity against various types of leukemia by several mechanisms of a |
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