A Bcr-Abl kinase inhibitor (IC50 = 5.8 nM) that is 25- to 55-fold more potent than imatinib in vitro and ≥10-fold more potent in vivo; inhibits 12 out of the 13 most frequent imatinib-resistant Bcr-Abl point mutations

Bafetinib – 10 mg

Brand:
Cayman
CAS:
859212-16-1
Storage:
-20
UN-No:
Non-Hazardous - /

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 (Item No. 13139), with modifications added to improve binding and potency against Bcr-Abl kinase (IC50 = 5.8 nM).{30982} It is 25- to 55-fold more potent than imatinib in vitro and ≥10-fold more potent in vivo.{30982} 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.{30982}  

 

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Description

A Bcr-Abl kinase inhibitor (IC50 = 5.8 nM) that is 25- to 55-fold more potent than imatinib in vitro and ≥10-fold more potent in vivo; inhibits 12 out of the 13 most frequent imatinib-resistant Bcr-Abl point mutations, but not the T315I mutation; also targets the Src family kinase Lyn (IC50 = 19 nM)

Formal name: N-[3-([4,5′-bipyrimidin]-2-ylamino)-4-methylphenyl]-4-[[(3S)-3-(dimethylamino)-1-pyrrolidinyl]methyl]-3-(trifluoromethyl)-benzamide

Synonyms:  INNO-406|NS-187

Molecular weight: 576.6

CAS: 859212-16-1

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Abl Family & Bcr-Abl||Product Type|Biochemicals|Kinase Inhibitors|SRC Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Abl family & Bcr-Abl Signaling||Research Area|Cancer|Cell Signaling|SRC Family Signaling

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