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]
|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 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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 70 mg/mL|
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