PD0166285 dihydrochloride是 P-gp 的一个底物，是WEE1抑制剂，也可微弱抑制Myt1，IC50值分别为 24 和 72 nM。PD0166285 dihydrochloride 对 Chk1 的 IC50值为3.433 μM。
| 生物活性 | PD0166285 dihydrochloride, a substrate of P-gp, is aWEE1inhibitor and a weakMyt1inhibitor withIC50values of 24 and 72 nM, respectively. PD0166285 dihydrochloride exhibits an IC50of 3.433 μM forChk1[1]. |
| IC50& Target | IC50: 24 nM (WEE1), 72 nM (Myt1), 3.433 μM (Chk1)[1]. |
体外研究
(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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体内研究
(In Vivo) | | Animal Model: | Wild-type, Abcg2-/-, Abcb1a/b-/-and Abcb1a/b;Abcg2-/-FVB mice[2]. | | Dosage: | 5 mg/kg. | | Administration: | IV. | | Result: | Cmaxis about 400 ng/mL.
P-gp, but not BCRP, limited the brain penetration of PD0166285. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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