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| Bafetinib Basic information |
| Bafetinib Chemical Properties |
| Melting point | 166-168°C | | density | 1.36±0.1 g/cm3(Predicted) | | storage temp. | Refrigerator | | pka | 12.72±0.70(Predicted) |
| Bafetinib Usage And Synthesis |
| Description | Bcr-Abl, a fusion protein with deregulated tyrosine kinase activity, is highly expressed in chronic myelogenous leukemia (CML). Bafetinib is a rationally developed tyrosine kinase inhibitor based on the chemical structure of imatinib , with modifications added to improve binding and potency against Bcr-Abl kinase (IC50 = 5.8 nM). It is 25- to 55-fold more potent than imatinib in vitro and ≥10-fold more potent in vivo. Bafetinib inhibits 12 out of the 13 most frequent imatinib-resistant Bcr-Abl point mutations, but not the T315I mutation and also targets the Src family kinase Lyn (IC50 = 19 nM), which has been associated with resistance to imatinib in CML. | | Chemical Properties | Pale Yellow Solid | | Uses | A substituted benzamide derivative structurally related to STI-571 (Imatinib Mesylate). It was identified as highly potent Bcr-Abl kinase inhibitor. |
| Bafetinib Preparation Products And Raw materials |
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