Size | Price | Stock |
---|---|---|
5mg | $55 | In-stock |
10mg | $90 | In-stock |
25mg | $150 | In-stock |
50mg | $250 | In-stock |
100mg | $400 | In-stock |
200 mg | Get quote | |
500 mg | Get quote | |
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Cat. No. : | HY-11001 |
M.Wt: | 361.48 |
Formula: | C19H31N5O2 |
Purity: | >98 % |
Solubility: | DMSO : ≥ 50 mg/mL (138.32 mM) |
PHA-793887 is a potent, ATP-competitive CDK inhibitor, can inhibit Cdk2, Cdk1, Cdk4, and Cdk9 with IC50s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen synthase kinase 3β with an IC50 of 79 nM.
IC50 & Target: IC50: 8 nM (Cdk2), 60 nM (Cdk1), 62 nM (Cdk4) 138 nM (Cdk9), 79 nM (GSK-3β)[1][4], 5 nM (CDK5/p25), 10 nM (CDK7/cyclin H)[4]
Ki: 8 nM (CDK2/Cyclin A)[2]
In Vitro: PHA-793887 partially inhibits Rb phosphorylation at 1 μM and almost completely at 3 μM, in A2780 tumor cell line. PHA-793887 (1 μM) partially inhibits phosphorylation of the Cdk2 substrates Rb and NPM in A2780 tumor cell line. PHA-793887 (6 μM) significantly inhibits Rb and NPM phosphorylation in MCF7 cell line[1]. PHA-793887 shows cytotoxic activities against leukemic cell lines in vitro, with IC50 ranging from 0.3 to 7 μM. In colony assays, PHA-793887 is highly cytotoxic for leukemia cell lines, with an IC50 <0.1 μM. PHA-793887 induces cell-cycle arrest, inhibits Rb and nucleophosmin phosphorylation, and modulates cyclin E and cdc6 expression at low doses of 0.2 to 1 μM and induces apoptosis at the highest dose of 5 μM. PHA-793887 is a novel inhibitor of several cdk, including cdk1, cdk2, cdk4, cdk5, cdk7, and cdk9 with IC50 in the 5 to 140 nM range[3].
In Vivo: PHA-793887 induces tumor growth inhibition in the range of 50% at dose of 15 mg/kg to 75% at dose of 30 mg/kg in CD-1 nude mice. PHA-793887 (30 mg/kg, i.v.) also induces significant downregulation of the 58-gene panel in the skin of CD-1 mice[1]. PHA-793887 (20 mg/kg, i.v.) induces tumor regression in the HL60 model. In the K562 model, PHA-793887 significantly reduces tumor growth. Moreover, PHA-793887 (20 mg/kg, i.v.) inhibits human primary leukemia growth in engraftment setting in vivo[3].
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