Bafetinib Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
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 (IC
50 = 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 (IC
50 = 19 nM), which has been associated with resistance to imatinib in CML.
Chemische Eigenschaften
Pale Yellow Solid
Verwenden
A substituted benzamide derivative structurally related to STI-571 (Imatinib Mesylate). It was identified as highly potent Bcr-Abl kinase inhibitor.
Bafetinib Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
