PD0166285

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PD0166285  纯度: 99.46%

PD0166285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 对 Chk1 的IC50 值为 3.433 μM。

PD0166285

PD0166285 Chemical Structure

CAS No. : 185039-89-8

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1691 In-stock
5 mg ￥1500 In-stock
10 mg ￥2400 In-stock
25 mg ￥5400 In-stock
50 mg ￥9400 In-stock
100 mg 询价

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PD0166285 相关产品

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生物活性

PD0166285, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC50 values of 24 and 72 nM, respectively. PD0166285 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

512.43

Formula

C26H27Cl2N5O2
CAS 号

185039-89-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 65 mg/mL (126.85 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9515 mL 9.7574 mL 19.5149 mL
5 mM 0.3903 mL 1.9515 mL 3.9030 mL
10 mM 0.1951 mL 0.9757 mL 1.9515 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: 2.17 mg/mL (4.23 mM); Clear solution; Need warming

    此方案可获得 2.17 mg/mL (4.23 mM) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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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