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Purity: ≥98%
Avasimibe (CI-1011; PD 148515; CI1011; CI 1011; PD148515; PD-148515) is a novel, potent and orally bioavailable inhibitor of acyl-Coenzyme A:cholesterol acyltransferase (ACAT) with the potential for the treatment of atherosclerosis and hyperlipidaemia. It inhibits ACAT1/2 with IC50s of 24 and 9.2 µM, respectively. It also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively.
| ln Vitro |
Prostate cancer (PCa) cells proliferate less when avasimibe (0, 0.25, 5, 10, 20, 40, and 80 μM; 1, 2 and 3 days) is administered [2]. The expression of β-catenin, Vimentin, N-cadherin, Snail, and MMP9—all of which are closely linked to the epithelial-mesenchymal transition (EMT)—is reduced by avasimibe (10 and 20 μM; 48 hours) [2]. In prostate cancer, avasimibe (10 and 20 μM) induces cell cycle arrest via the E2F-1 signaling pathway. In PCa cells, avasimibe causes a G1 phase cell cycle arrest [2]. PCa cell metastasis is inhibited by avasimibe (10 and 20 μM) [2].
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| ln Vivo |
For seven weeks, avasimibe (30 mg/kg intraperitoneally every other day) suppresses the development and metastasis of PCa cells in vivo. Avasimibe is minimal in toxicity and has good biocompatibility [2].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: PCa cells (PC-3 and DU 145) Tested Concentrations: 0, 0.25, 5, 10, 20, 40 and 80 µM Incubation Duration: 1, 2, and 3 days Experimental Results: Dose dependently inhibited PC-3 and DU 145 cell viability. Western Blot Analysis[2] Cell Types: PCa cells (PC-3 and DU 145) Tested Concentrations: 10 and 20 µM Incubation Duration: 48 hrs (hours) Experimental Results: decreased protein levels of EMT-related proteins ( β-catenin, Vimentin, N-cadherin, Snail, MMP9 and E-cadherin). Cell Cycle Analysis[2] Cell Types: PCa cells (PC-3 and DU 145) Tested Concentrations: 10 and 20 µM Incubation Duration: 48 hrs (hours) Experimental Results: Induced G1 phase cycle arrest and altered the G1 phase-related protein levels in PCa cells. |
| Animal Protocol |
Animal/Disease Models: SPF male mice (BALB/c-nude, 4 weeks old) bearing PCa cells[2]
Doses: 30 mg/kg Route of Administration: Intraperitoneally injected for 7 weeks Experimental Results: decreased tumor volume compared with that of the control group. Inhibited PCa growth and migration in vivo. |
| References |
[1]. Taichi Ohshiro,et al. Pyripyropene A, an acyl-coenzyme A:cholesterol acyltransferase 2-selective inhibitor, attenuates hypercholesterolemia and atherosclerosis in murine models of hyperlipidemia. Arterioscler Thromb Vasc Biol. 2011 May;31(5):1108-15.
[2]. Kangping Xiong, et al. The cholesterol esterification inhibitor avasimibe suppresses tumour proliferation and metastasis via the E2F-1 signalling pathway in prostate cancer.Cancer Cell Int. 2021 Aug 30;21(1):461. |
| Molecular Formula |
C29H43NO4S
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| Molecular Weight |
501.72
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| CAS # |
166518-60-1
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| Related CAS # |
166518-61-2 (sodium);166518-60-1 (free form);
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| SMILES |
c1(C(C)C)cc(cc(c1CC(NS(Oc1c(cccc1C(C)C)C(C)C)(=O)=O)=O)C(C)C)C(C)C
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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