Bafetinib

Bafetinib 화학적 특성, 용도, 생산

• 개요

  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.

• 화학적 성질

  Pale Yellow Solid

• 용도

  A substituted benzamide derivative structurally related to STI-571 (Imatinib Mesylate). It was identified as highly potent Bcr-Abl kinase inhibitor.

Bafetinib 공급 업체

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