A potent inhibitor of Cdk1

AZD 5438 – 50 mg

Brand:
Cayman
CAS:
602306-29-6
Storage:
-20
UN-No:
Non-Hazardous - /

AZD 5438 is a potent inhibitor of the cyclin-dependent kinases (CDKs) 1, 2, and 9 (IC50s = 16, 6, and 20 nM, respectively).{38013} AZD 5438 also inhibits the kinase activity of Cdk5/p25 and glycogen synthase kinase 3β (GSK3β) (IC50s = 14 and 17 nM, respectively). AZD 5438 induces cell cycle arrest by inhibiting phosphorylation of CDK-dependent substrates and exhibits in vitro antiproliferative activity against a range of tumor cell lines including lung, colorectal, breast, prostate, and hematologic tumors with IC50s ranging from 200 nM (MCF-7) to 1,700 nM (ARH-77).{38013,38014} AZD 5438 inhibits growth of human tumor xenografts derived from a wide range of cancer types and inhibits cell cycle proteins.{38013,38015}  

 

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Description

A potent inhibitor of Cdk1, Cdk2, and Cdk9 (IC50s = 16, 6, and 20 nM, respectively); inhibits kinase activity of Cdk5/p25 and GSK3β; induces cell cycle arrest by inhibiting phosphorylation of CDK-dependent substrates; has in vivo antiproliferative activity against a range of tumor cell lines (IC50s ranging from 200-1,700 nM); in vivo oral administration inhibits growth of human tumor xenografts and inhibits cell cycle proteins

Formal name: 4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine

Synonyms: 

Molecular weight: 371.5

CAS: 602306-29-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|CDKs||Product Type|Biochemicals|Kinase Inhibitors|GSK3||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Signaling|GSK3 Signaling

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