185039-89-8

185039-89-8 structure

Name: PD0166285
Chemical Name: PD166285
CAS Number: 185039-89-8
Molecular Formula: C₂₆H₂₇Cl₂N₅O₂
Molecular Weight: 512.431
Catalog: Signaling Pathways Cell Cycle/DNA Damage Wee1
Create Date: 2018-06-11 05:30:39
Modify Date: 2024-01-22 20:38:37
PD0166285 is a WEE1 inhibitor and a weak Myt1 inhibitor with IC50s of 24 and 72 nM, respectively.

Name	PD166285
Synonyms	PD166285 TCMDC-140940 6-(2,6-Dichlorophenyl)-2-({4-[2-(diethylamino)ethoxy]phenyl}amino)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-(2,6-dichlorophenyl)-2-[[4-[2-(diethylamino)ethoxy]phenyl]amino]-8-methyl- 6-(2,6-Dichlorophenyl)-2-[[4-[2-(diethylamino)ethoxy]phenyl]amino]-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one PD0166285

Description	PD0166285 is a WEE1 inhibitor and a weak Myt1 inhibitor with IC50s of 24 and 72 nM, respectively.
Related Catalog	Signaling Pathways >> Cell Cycle/DNA Damage >> Wee1 Research Areas >> Cancer
Target	IC50: 24 nM (WEE1), 72 nM (Myt1)[1]
In Vitro	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].
Cell Assay	For PA-1 cell clonogenic assay, growing cells are irradiated with the indicated dose of γ-radiation (2–8 Gy). Cells are subsequently cultured in the original medium for 12 h, followed by treatment of 0.4 μM PD0166285 or DMSO control for another 4 h[1].
References	[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.