A selective second generation Bcr-Abl tyrosine kinase inhibitor (IC50 = 30.6 nM); targets PDGFRα and β (IC50s = 75.5 and 130 nM

Radotinib – 1 mg

Brand:
Cayman
CAS:
926037-48-1
Storage:
-20
UN-No:
Non-Hazardous - /

Radotinib is a selective second generation tyrosine kinase inhibitor that targets both the wild-type and mutant forms of Bcr-Abl, with an IC50 value of 30.6 nM in Ba/F3 human chronic myeloid leukemia cells expressing the wild-type form.{38002} Radotinib also inhibits platelet-derived growth factor receptors (PDGFRs) α and β with IC50 values of 75.5 and 130 nM, respectively.{38000,38001} Binding of radotinib to Bcr-Abl in vitro inhibits the phosphorylation of the downstream signaling mediator CrkL.{38001} In acute myeloid leukemia cells, in vitro treatment with radotinib at doses of 10-100 µM reduces viability, activates the mitochondrial apoptosis pathway, and promotes expression of the differentiation marker CD11b.{38000}  

 

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Description

A selective second generation Bcr-Abl tyrosine kinase inhibitor (IC50 = 30.6 nM); targets PDGFRα and β (IC50s = 75.5 and 130 nM, respectively); reduces viability and promotes differentiation in human acute myeloid leukemia cells,

Formal name: 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(2-pyrazinyl)-2-pyrimidinyl]amino]-benzamide

Synonyms:  IY-5511

Molecular weight: 530.5

CAS: 926037-48-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Abl Family & Bcr-Abl||Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|Abl family & Bcr-Abl Signaling||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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