PD0166285 dihydrochloride

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PD0166285 dihydrochloride 

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。

PD0166285 dihydrochloride

PD0166285 dihydrochloride Chemical Structure

CAS No. : 212391-63-4

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PD0166285 dihydrochloride 的其他形式现货产品:

PD0166285

生物活性

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].

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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: Cmax is about 400 ng/mL.
P-gp, but not BCRP, limited the brain penetration of PD0166285.

分子量

585.35

Formula

C26H29Cl4N5O2
CAS 号

212391-63-4
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.
参考文献

  • [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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