SP-141 是一种特异性的MDM2抑制剂。SP-141 促进 MDM2 自泛素化和降解。SP-141 可用于胰腺癌和乳腺癌的研究。
| 生物活性 | SP-141 is a specific inhibitor ofMDM2. SP-141 promotesMDM2auto-ubiquitination and degradation. SP-141 might be used for the research of pancreaticcancerand breastcancercells[1]. |
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体外研究
(In Vitro) | SP-141 (0.01-10 μM; 72 hours) inhibits human pancreatic cancer cell growth with IC50values of less than 0.5 μM (0.38-0.50 μM) in a p53-independent manner. The IMR90 cells are much less sensitive to SP141 than the pancreatic cancer cells, suggesting that SP141 has a selective cytotoxicity for cancer cells[1].
SP141 induces MDM2 auto-ubiquitination and proteasomal degradation in both HPAC and Panc-1 cells[1].
Cell Viability Assay[1] | Cell Line: | HPAC, Panc-1, AsPC-1, and Mia-Paca-2 pancreatic cancer cell lines. Human primary fibroblasts (IMR90) | | Concentration: | 0.01, 0.1, 1, and 10 μM | | Incubation Time: | 72 hours | | Result: | IC50s of 0.38, 0.50, 0.36, 0.41, and 13.22 μM for HPAC, Panc-1, AsPC-1, Mia-Paca-2, and IMR90, respectively. |
Western Blot Analysis[1] | Cell Line: | HPAC and Panc-1 cells | | Concentration: | 0.5 μM | | Incubation Time: | 120 minutes | | Result: | Reduced the MDM2 protein levels.
Increased the degradation rate of the MDM2 protein in the presence of Cycloheximide (15 μg/mL). |
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体内研究
(In Vivo) | SP-141 (40 mg/kg; administered by i.p. injection; 5 d/wk for about three weeks) suppresses pancreatic tumor growth in both xenograft and orthotopic mouse models[1].
| Animal Model: | Nude mice bearing Panc-1 xenograft tumors[1] | | Dosage: | 40 mg/kg | | Administration: | Administered by i.p. injection; 5 d/wk for about three weeks | | Result: | Significantly suppressed the growth of pancreatic xenograft tumors. On Day 18, the tumor volume in the treated group was reduced by 75% compared with that in the control group. There were no significant differences in the body weight compared with the control group. |
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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 : 125 mg/mL(385.35 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.0828 mL | 15.4140 mL | 30.8280 mL | | 5 mM | 0.6166 mL | 3.0828 mL | 6.1656 mL | | 10 mM | 0.3083 mL | 1.5414 mL | 3.0828 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: ≥ 2.08 mg/mL (6.41 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.41 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (6.41 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.41 mM，饱和度未知) 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 20.8 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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