PHA-848125

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP01918CAS No. ：802539-81-7Purity：98%

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CAS No.	802539-81-7	Cat. No.	BCP01918
Name	PHA-848125
Synonyms	PHA 848125;PHA848125;Milciclib;
SMILES
Chemical Name
Formula	C25H32N8O	M. Wt	460.57
Purity	98%	Storage	Store at 4-8°C
Description	PHA-848125 inhibits, although with lower potency, the activities of cyclin H/CDK7, cyclin D1/CDK4, p35/CDK5, as well as cyclin E/CDK2 and cyclin B/CDK1 with IC50 values of 0.15, 0.16, 0.265, 0.363, 0.398 μM, respectively.Thropomyosin receptor kinase A is also inhibited by PHA-848125 in the same nanomolar range as CDKs. In the most PHA-848125-sensitive cell line, PHA-848125 induces a concentration-dependent G(1) arrest.[2] PHA-848125 also impairs phosphorylation of the retinoblastoma protein at CDK2 and CDK4 specific sites, reduces retinoblastoma protein and cyclin A levels, and increases p21(Cip1), p27(Kip1) and p53 expression. PHA-848125 is added to the cells 48 h after TMZ and cell growth is evaluated after 3 additional days of culture. [2] A drug combination of TMZ, BG and PHA-848125 induces an additive or synergistic effect on cell growth, depending on the cell line. [2] In the absence of BG, the combination is still more active than the single agents in cell lines moderately sensi