Description
PHA-848125 can inhibit cyclin A/CDK2, cyclin H/CDK7,cyclin D1/CDK4,p35/CDK5, and cyclin E/CDK2 with IC50 of 45 nM, 150 nM, 160 nM, 265 nM and 363 nM.
Storage
2 years at -20centigrade Powder
Targets
cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, p35/CDK5, cyclin E/CDK2
Molecular Formula
C25H32N8O
Chemical Name
N,1,4,4-tetramethyl-8-(4-(4-methylpiperazin-1-yl)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
In vitro
PHA-848125 is a potent dual inhibitor of CDKs and TRKs, possesses significant antitumor activity. PHA-848125 can inhibit cell proliferation of a wide panel of tumoral cell lines with submicromolar IC(50). PHA-848125-treated cells show cell cycle arrest in G(1) and reduced DNA synthesis, accompanied by inhibition of pRb phosphorylation and modulation of other CDK-dependent marker
In vivo
Following oral administration, PHA-848125 has significant antitumor activity in various human xenografts and carcinogen-induced tumors as well as in disseminated primary leukemia models, with plasma concentrations in rodents in the same range as those found active in inhibiting cancer cell proliferation.
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