PD0166285 |
| Katalog-Nr.GC32853 |
PD0166285, ein Substrat von P-gp, ist ein WEE1-Inhibitor und ein schwacher Myt1-Inhibitor mit IC50-Werten von 24 bzw. 72 nM. PD0166285 weist einen IC50 von 3,433 μM fÜr Chk1 auf.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 185039-89-8
Sample solution is provided at 25 µL, 10mM.
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PD0166285 is a WEE1 inhibitor and a weak Myt1 inhibitor with IC50s of 24 and 72 nM, respectively.
PD0166285 is a pyridopyrimidine class of molecule. At the cellular level, 0.5 μM PD0166285 dramatically inhibits irradiation-induced Cdc2 phosphorylation at the Tyr-15 and Thr-14 in seven of seven cancer cell lines. 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. Biologically, PD0166285 acts as a radiosensitizer to sensitize cells to radiation-induced cell death with a sensitivity enhancement ratio of 1.23[1].
[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.
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