PD0166285 dihydrochloride

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

PD0166285 dihydrochloride 

PD0166285 dihydrochloride是 P-gp 的一个底物,是 WEE1 抑制剂,也可微弱抑制 Myt1IC50 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

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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].

上海金畔生物科技有限公司 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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务