PD0166285PD0166285
MedChemExpress (MCE)
HY-13925
185039-89-8
99.46%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
PD0166285, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC50 values of 24 and 72 nM, respectively. PD0166285 exhibits an IC50 of 3.433 μM for Chk1.
PD0166285 (0.5 μM) dramatically inhibits irradiation-induced Cdc2 phosphorylation at the Tyr-15 and Thr-14 in seven of seven cancer cell lines[1].?PD0166285 sensitizes radiation-induced cell killing in p53 mutant HT29 cells and in the E6-transfected, p53-null ovarian cancer cell line PA-1 but to a lesser extent in p53 wild-type PA-1 cells. PD0166285 abrogates irradiation-induced G2 arrest and significantly increases mitotic cell populations[1].?PD0166285 acts as a radiosensitizer to sensitize cells to radiation-induced cell death with a sensitivity enhancement ratio of 1.23[1].
Animal Model: Wild-type, Abcg2-/-, Abcb1a/b-/- and Abcb1a/b
Abcg2-/- FVB mice[2]. Dosage: 5 mg/kg. Administration: IV. Result: Cmax is about 400 ng/mL. P-gp, but not BCRP, limited the brain penetration of PD0166285. Molecular Weight 512.43
IC50: 24 nM (WEE1), 72 nM (Myt1), 3.433 μM (Chk1)[1]. Cellular Effect Cell Line Type Value Description References
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[1]. Wang Y, et al. Radiosensitization of p53 mutant cells by PD0166285, a novel G(2) checkpoint abrogator. Cancer Res. 2001 Nov 15
61(22):8211-7. [Content Brief]
[2]. Mark C de Gooijer, et al. ATP-binding cassette transporters limit the brain penetration of Wee1 inhibitors. Invest New Drugs. 2018 Jun
36(3):380-387. [Content Brief]