biological activity | PD0166285 dihyaloride is a substrate of P-gp, which is a WEE1 inhibitor and also weakly inhibits Myt1,IC50 values were 24 and 72 nM, respectively. The IC50 value of PD0166285 dihydrochloride for Chk1 was 3.433 μm. |
Target | IC50: 24 nM (WEE1), 72 nM (Myt1), 3.433 μm (Chk1). |
Cell Line:
| Human and mouse cancer cell lines (HCT116, HT29, DLD-1, HCT8, H460, HeLa, C 26). |
Concentration:
| 0.5 μM. |
Incubation Time:
| 4 h. |
Result:
| Inhibited Cdc2Y15 and CdcT14 phosphorylation. C max is about 400 ng/mL. P-gp, but not BCRP, limited the brain penetration of PD0166285. |
Animal Model:
| Wild-type, Abcg2 -/- , Abcb1a/b -/- and Abcb1a/b;Abcg2 -/- FVB mice. |
Dosage:
| 5 mg/kg. |
Administration:
| IV. |