PHA-848125

Short Summary : CDK inhibitor,potent and ATP-competitive

Category : Cell Cycle/Checkpoint|Cyclin-Dependent Kinases

Purity : 0.98

CAS Number : 802539-81-7

Formula : C25H32N8O

Molecular Weight :

Molecular Weight : 460.57

SMILE : CC1(CC2=CN=C(N=C2C3=C1C(=NN3C)C(=O)NC)NC4=CC=C(C=C4)N5CCN(CC5)C)C

Solubility : >23.1mg/mL in DMSO

Storage : Store at -20°C

Description : PHA-848125 is a potent and ATP-competitive Cdk2/cyclin A inhibitor with an IC50 value of 45 nM. PHA-848125 also inhibited Cdk7/cyclin H, Cdk4/cyclin D1, Cdk5/p35, Cdk2/cyclin E and Cdk1/cyclin B with less potency (IC50= 0.15 M, 0.16 M, 0.265 M, 0.363 M and 0.398 M, respectively). [1]
CDK (cyclin-dependent kinase) is a group of serine/threonine kinases. It is activated by binding to cyclin and participates in the regulation of cell cycle.
In cells treated with PHA-848125, hyperphosphorylated form of CDK substrateretinoblastoma protein (pRb) was reduced and hypophosporylated from of pRb was accumulated. It further indicated inhibition effect of PHA-848125 on CDK2 activity. [1]
In human ovarian A2780 xenogaft mouse model, 20, 30 and 40mg/kg of PHA-848125 were each administrated orally twice a day for 10 days. PHA-848125 inhibited A2780 tumor growth up to 91% at 40 mg/kg dose. [1]
Reference:1. Brasca MG, Amboldi N, Ballinari D et al. Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor. J Med Chem. 2009 Aug 27;52(16):5152-63.

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