PHA-848125 (Synonyms: Milciclib) |
| Catalog No.GC15588 |
PHA-848125 (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.
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Cas No.: 802539-81-7
Sample solution is provided at 25 µL, 10mM.
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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 µM, 0.16 µM, 0.265 µM, 0.363 µM and 0.398 µM, 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 substrate—retinoblastoma 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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