Avasimibe (CI-1011; PD-148515) 是一种有效的，具有口服活性的酰基辅酶 A: 胆固醇酰基转移酶 (ACAT) 抑制剂，对ACAT1和ACAT2的IC50分别为 24 和 9.2 μM。Avasimibe 可用于前列腺癌的研究。
| 生物活性 | Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterolacyltransferase(ACAT; also calledSOAT)) inhibitor withIC50s of 24 and 9.2 μM forACAT1andACAT2, respectively[1]. Avasimibe can be used for the research of prostatecancer[2]. |
| IC50& Target[1] | ACAT1 24 μM (IC50) | ACAT2 9.2 μM (IC50) |
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体外研究
(In Vitro) | Avasimibe (0, 0.25, 5, 10, 20, 40 and 80 μM; for 1, 2, and 3 days) reduces proliferation in the prostate cancer (PCa) cells[2].
Avasimibe (10 and 20 μM; 48 h) reduces the expression of β-catenin, Vimentin, N-cadherin, Snail and MMP9, which are tightly associated with epithelial-mesenchymal transition (EMT)[2].
Avasimibe (10 and 20 μM) trigger cell cycle arrest via the E2F-1 signalling pathway in prostate cancer. Avasimibe induces G1 phase cell cycle arrest of PCa cells[2].
Avasimibe (10 and 20 μM) inhibits the metastasis of PCa cells[2].
Cell Viability Assay[2] | Cell Line: | PCa cells (PC-3 and DU 145) | | Concentration: | 0, 0.25, 5, 10, 20, 40 and 80 μM | | Incubation Time: | 1, 2, and 3 days | | Result: | Dose dependently inhibited PC-3 and DU 145 cell viability. |
Western Blot Analysis[2] | Cell Line: | PCa cells (PC-3 and DU 145) | | Concentration: | 10 and 20 μM | | Incubation Time: | 48 hours | | Result: | Reduced protein levels of EMT-related proteins (β-catenin, Vimentin, N-cadherin, Snail, MMP9 and E-cadherin). |
Cell Cycle Analysis[2] | Cell Line: | PCa cells (PC-3 and DU 145) | | Concentration: | 10 and 20 μM | | Incubation Time: | 48 hours | | Result: | Induced G1 phase cycle arrest and altered the G1 phase-related protein levels in PCa cells. |
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体内研究
(In Vivo) | Avasimibe (30 mg/kg, intraperitoneally injected on alternate days for 7 weeks) suppresses PCa cell growth and metastasis in vivo. Avasimibe has good biocompatibility and low toxicity[2].
| Animal Model: | SPF male mice (BALB/c-nude, 4 weeks old) bearing PCa cells[2] | | Dosage: | 30 mg/kg | | Administration: | Intraperitoneally injected for 7 weeks | | Result: | Reduced tumour volume compared with that of the control group. Inhibited PCa growth and migration in vivo. |
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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 : 100 mg/mL(199.31 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9931 mL | 9.9657 mL | 19.9314 mL | | 5 mM | 0.3986 mL | 1.9931 mL | 3.9863 mL | | 10 mM | 0.1993 mL | 0.9966 mL | 1.9931 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: 7.5 mg/mL (14.95 mM); Suspended solution; Need ultrasonic
此方案可获得 7.5 mg/mL (14.95 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 75.0 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% (20%SBE-β-CDin saline) Solubility: 7.5 mg/mL (14.95 mM); Suspended solution; Need ultrasonic
此方案可获得 7.5 mg/mL (14.95 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 75.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: 7.5 mg/mL (14.95 mM); Clear solution; Need ultrasonic
此方案可获得 7.5 mg/mL (14.95 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 75.0 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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