An ATP-competitive Chk1 inhibitor (Ki = 0.49 nM) that demonstrates 100-fold selectivity over Chk2; abrogates DNA damage-induced cell cycle arrest in tumor cell lines and xenografts

PF-477736 – 50 mg

Brand:
Cayman
CAS:
952021-60-2
Storage:
-20
UN-No:
Non-Hazardous - /

Checkpoint kinase 1 (Chk1) regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. PF-477736 is an ATP-competitive inhibitor of Chk1 with a Ki value of 0.49 nM that demonstrates 100-fold selectivity over Chk2.{29021} When used in combination with various chemotherapeutics, PF-477736 abrogates DNA damage-induced cell cycle arrest, potentiating the antiproliferative effects of these compounds in tumor cell lines and xenografts.{29021,29022,29023}  

 

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Description

An ATP-competitive Chk1 inhibitor (Ki = 0.49 nM) that demonstrates 100-fold selectivity over Chk2; abrogates DNA damage-induced cell cycle arrest in tumor cell lines and xenografts, potentiating the antiproliferative effects of various chemotherapeutics

Formal name: (αR)-amino-N-[5,6-dihydro-2-(1-methyl-1H-pyrazol-4-yl)-6-oxo-1H-pyrrolo[4,3,2-ef][2,3]benzodiazepin-8-yl]-cyclohexaneacetamide

Synonyms: 

Molecular weight: 419.5

CAS: 952021-60-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Checkpoint Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Signaling||Research Area|Cancer|DNA Damage and Repair

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