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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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