PD0166285 dihydrochloride 

PD0166285 dihydrochloride, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC₅₀ values of 24 and 72 nM, respectively. PD0166285 dihydrochloride exhibits an IC₅₀ of 3.433 μM for Chk1^[1].

IC50: 24 nM (WEE1), 72 nM (Myt1), 3.433 μM (Chk1)^[1].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

585.35

C₂₆H₂₉Cl₄N₅O₂

212391-63-4

O=C1N(C)C2=NC(NC3=CC=C(OCCN(CC)CC)C=C3)=NC=C2C=C1C4=C(Cl)C=CC=C4Cl.[H]Cl.[H]Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]