Inhibits Cdk2/cyclin A

PHA-793887 – 1 mg

Brand:
Cayman
CAS:
718630-59-2
Storage:
-20
UN-No:
Non-Hazardous - /

PHA-793887 is a pyrrolo[3,4-c]pyrazole that inhibits cyclin-dependent kinases Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p25, and Cdk7/cyclin H with IC50 values of 8, 8, 5, and 10 nM, respectively.{30703} It is more than 6-fold selective for these kinases over Cdk1/cyclin B, Cdk4/cyclin D1, Cdk9/cyclin T, and GSK3β (IC50s = 60, 62, 138, and 79 nM, respectively).{30703} PHA-793887 is cytotoxic to human ovarian A2780, colon HCT116, pancreatic BX-PC3, and leukemic K562, KU812, KCL22, and TOM1 cells both in vitro and in xenograft models.{30703,30704} This compound has been examined in patients with solid tumors in phase 1 clinical trials.{30702}  

 

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Description

Inhibits Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p25, and Cdk7/cyclin H with IC50 values of 8, 8, 5, and 10 nM, respectively; cytotoxic to human ovarian A2780, colon HCT116, pancreatic BX-PC3, and leukemic K562, KU812, KCL22, and TOM1 cells both in vitro and in xenograft models

Formal name: 3-methyl-N-[1,4,5,6-tetrahydro-6,6-dimethyl-5-[(1-methyl-4-piperidinyl)carbonyl]pyrrolo[3,4-c]pyrazol-3-yl]-butanamide

Synonyms: 

Molecular weight: 361.5

CAS: 718630-59-2

Purity: ≥95%

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 Death||Research Area|Cancer|Cell Signaling

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