212391-63-4

212391-63-4 structure

Name: PD 166285 dihydrochloride
Chemical Name: 6-(2,6-dichlorophenyl)-2-[4-[2-(diethylamino)ethoxy]anilino]-8-methylpyrido[2,3-d]pyrimidin-7-one,dihydrochloride
CAS Number: 212391-63-4
Molecular Formula: C₂₆H₂₈Cl₃N₅O₂
Molecular Weight: 548.89200
Catalog: Pharmaceutical intermediate Heterocyclic compound Pyridine compound Ethylpyridine
Create Date: 2019-01-21 11:33:04
Modify Date: 2024-04-09 19:13:36
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].

Name	6-(2,6-dichlorophenyl)-2-[4-[2-(diethylamino)ethoxy]anilino]-8-methylpyrido[2,3-d]pyrimidin-7-one,dihydrochloride
Synonyms	Heparin-Cantithrombin III

Description	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].
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> Cell Cycle/DNA Damage >> Wee1
Target	IC50: 24 nM (WEE1), 72 nM (Myt1), 3.433 μM (Chk1)[1].
In Vitro	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]. Western Blot Analysis[1] Cell Line: Human and mouse cancer cell lines (HCT116, HT29, DLD-1, HCT8, H460, HeLa, C 26). Concentration: 0.5 μM. Incubation Time: 4 h. Result: Inhibited Cdc2Y15 and CdcT14 phosphorylation.
In Vivo	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.
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. [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.

Melting Point	239-242?C
Molecular Formula	C₂₆H₂₈Cl₃N₅O₂
Molecular Weight	548.89200
Exact Mass	547.13100
PSA	72.28000
LogP	6.64150
Storage condition	Desiccate at RT

Hazard Codes	Xi

212391-63-4	1246814-59-4
1782532-06-2	250717-55-6
172548-79-7	199850-67-4
1675203-84-5	2667680-33-1
172519-48-1	162682-14-6
1158522-08-7	940364-43-2
134104-43-1	131615-57-1
6906-52-1	2229574-40-5
930439-75-1	1018584-77-4
1375289-11-4	849349-65-1