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PHA-793887 is a novel pan-cdk inhibitor, including cdk1, cdk2, cdk4, cdk5, cdk7, and cdk9 with IC50 in the 5 to 140 nM range. It is inactive against other 34 kinases representative of all kinase families, in particular c-abl, c-kit, lck, and TRKA with IC50＞10 mM. It shows anti-proliferative activity against several solid tumor cell lines, with IC50＜1 mM. In these cells, it is able to inhibit Rb phosphorylation and expression of S-phase cyclins, such as cyclin A. [1,2]
Front Oncol. 2022 Jul 28;12:968547.
Comprehensive analysis of the glutathione S-transferase Mu (GSTM) gene family in ovarian cancer identifies prognostic and expression significance
PHA-793887 purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | A2780 cells |
| Preparation method | Seeding cells into 96- or 384-wells plates at final concentration ranging from 1 ×104 to 3 ×104 per cm2. 24 hours later,using serial dilution of PHA-793887 to treat cells . At 72 hours after the treatment, using the CellTiter-Glo assay to evaluate the amount of cells . using a sygmoidal fit to calculate IC50 values |
| Concentrations | 0.1 nM-1 μM, dissolved in DMSO |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | Mouse xenograft models of human ovarian A2780, colon HCT-116 and pancreatic BX-PC3 carcinoma |
| Formulation | Dissolved in 5% dextrose solution |
| Dosages | 10, 20, and 30 mg/kg |
| Administration | Intravenous injection once daily |
| Molecular Weight | 361.48 |
| Formula | C19H31N5O2 |
| CAS Number | 718630-59-2 |
| Solubility (25°C) | DMSO 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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