A CDK inhibitor (IC50s = 0.017

CGP 60474 – 10 mg

Brand:
Cayman
CAS:
164658-13-3
Storage:
-20
UN-No:
- /

CGP 60474 is an inhibitor of cyclin-dependent kinases (CDKs; IC50s = 0.017, 0.08, and 0.05 µM for Cdk1/cyclin B, Cdk2/cyclin A, and Cdk2/cyclin E, respectively).{61149} It is selective for these CDKs over Cdk4/cyclin D1 (IC50 = 0.7 µM) and a variety of other kinases, including several PKC isoforms (IC50s = 1.9->100 µM), PKA (IC50 = 160 µM), and FLT1 (IC50 = 1 µM), among others, but does inhibit PKCα and v-Abl (IC50s = 0.25 and 0.4 µM, respectively). It inhibits proliferation of colon, breast, lung, prostate, and ovarian cancer cells (IC50s = 25-84, 21-280, 40 and 68, 17 and 20, and 18-38 nM, respectively). CGP 60474 also reduces LPS-induced IL-6, TNF-α, and RANTES secretion from J774.1 cells in a concentration-dependent manner and inhibits poly(I:C)-induced NF-κB nuclear translocation in the same cells when used at concentrations of 8 and 32 nM.{61150} It reduces plasma IL-6 levels and increases survival in a mouse model of LPS-induced endotoxemia when administered at a dose of 10 mg/kg.  

 

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Description

A CDK inhibitor (IC50s = 0.017, 0.08, and 0.05 µM for Cdk1/cyclin B, Cdk2/cyclin A, and Cdk2/cyclin E, respectively); selective for these CDKs over Cdk4/cyclin D1 (IC50 = 0.7 µM) and a variety of other kinases but does inhibit PKCα and v-Abl (IC50s = 0.25 and 0.4 µM, respectively); inhibits proliferation of colon, breast, lung, prostate, and ovarian cancer cells (IC50s = 25-84, 21-280, 40 and 68, 17 and 20, and 18-38 nM, respectively); inhibits poly(I:C)-induced NF-κB nuclear translocation in J774.1 cells at 8 and 32 nM; reduces plasma IL-6 levels and increases survival in a mouse model of LPS-induced endotoxemia at 10 mg/kg

Formal name: 3-[[4-[2-[(3-chlorophenyl)amino]-4-pyrimidinyl]-2-pyridinyl]amino]-1-propanol

Synonyms: 

Molecular weight: 355.8

CAS: 164658-13-3

Purity: ≥98%

Formulation: A solid

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