Products
Online Inquiry
Our Products Cannot Be Used As Medicines Directly For Personal Use.
Welcome! For price inquiries, please feel free to contact us through the form on the left side. We will get back to you as soon as possible.
PHA-848125
Cat No.
CEI-0307
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.
CAS No.
802539-81-7
Molecular Weight
460.57
Purity
>99%
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
Solubility
DMSO
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.
Download
Download Datasheet