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。
生物活性 | PD0166285, a substrate of P-gp, is aWEE1inhibitor and a weakMyt1inhibitor withIC50values of 24 and 72 nM, respectively. PD0166285 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 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(97.57 mM;Need ultrasonic) 配制储备液 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (4.88 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.88 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 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本网站选购。
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