PD0166285

Names

[ Name ]:
PD0166285

[Synonym ]:
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

Biological Activity

[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.

[Related Small Molecules]

Adavosertib (MK-1775)

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
665.3±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₆H₂₇Cl₂N₅O₂

[ Molecular Weight ]:
512.431

[ Flash Point ]:
356.2±34.3 °C

[ Exact Mass ]:
511.154175

[ LogP ]:
5.09

[ Vapour Pressure ]:
0.0±2.0 mmHg at 25°C

[ Index of Refraction ]:
1.637

[ Storage condition ]:
-20℃

[ Water Solubility ]:
Insuluble (4.9E-4 g/L) (25 ºC)

Related Compounds

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