Bafetinib Chemical Properties

Melting point:

166-168°C

Density 

1.36±0.1 g/cm3(Predicted)

storage temp. 

Refrigerator

solubility 

DMSO:42.0(Max Conc. mg/mL);72.84(Max Conc. mM)

form 

A crystalline solid

pka

12.72±0.70(Predicted)

color 

Light yellow to yellow

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(859212-16-1)Related Product Information

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