Introduction：Basic information about CAS 212391-63-4|PD 166285 dihydrochloride, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | PD 166285 dihydrochloride |
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| CAS Number | 212391-63-4 | Molecular Weight | 548.89200 |
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| Density | / | Boiling Point | / |
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| Molecular Formula | C26H28Cl3N5O2 | Melting Point | 239-242?C |
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| MSDS | / | Flash Point | / |
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Names
| Name | 6-(2,6-dichlorophenyl)-2-[4-[2-(diethylamino)ethoxy]anilino]-8-methylpyrido[2,3-d]pyrimidin-7-one,dihydrochloride |
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| Synonym | More Synonyms |
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PD 166285 dihydrochloride BiologicalActivity
| 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]. |
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| Related Catalog | Signaling Pathways >>Apoptosis >>ApoptosisResearch Areas >>CancerSignaling Pathways >>Cell Cycle/DNA Damage >>Wee1 |
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| Target | IC50: 24 nM (WEE1), 72 nM (Myt1), 3.433 μM (Chk1)[1]. |
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| 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. |
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| 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. |
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| 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. |
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Chemical & Physical Properties
| Melting Point | 239-242?C |
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| Molecular Formula | C26H28Cl3N5O2 |
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| Molecular Weight | 548.89200 |
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| Exact Mass | 547.13100 |
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| PSA | 72.28000 |
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| LogP | 6.64150 |
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| InChIKey | NADLBPWBFGTESN-UHFFFAOYSA-N |
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| SMILES | CCN(CC)CCOc1ccc(Nc2ncc3cc(-c4c(Cl)cccc4Cl)c(=O)n(C)c3n2)cc1.Cl.Cl |
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| Storage condition | Desiccate at RT |
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Safety Information
Synonyms
| Heparin-Cantithrombin III |
