2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. Avasimibe

Avasimibe  (Synonyms: CI-1011; PD-148515)

Cat. No.: HY-13215 Purity: 99.50%
COA Handling Instructions

Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively. Avasimibe can be used for the research of prostate cancer.

For research use only. We do not sell to patients.

Avasimibe Chemical Structure

Avasimibe Chemical Structure

CAS No. : 166518-60-1

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10 mM * 1 mL in DMSO USD 61 In-stock
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10 mg USD 55 In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

Avasimibe Related Antibodies

Top Publications Citing Use of Products

    Avasimibe purchased from MCE. Usage Cited in: Biomed Pharmacother. 2020 Oct;130:110508.  [Abstract]

    The effect of Avasimibe on the viability of T98 G is dose-dependent and time-dependent. Similar results are found in LN229 as well. Avasimibe has an anti-tumour effect on glioma.

    Avasimibe purchased from MCE. Usage Cited in: Biomed Pharmacother. 2020 Oct;130:110508.  [Abstract]

    qRT-PCR data showing the expression of linc00339 in T98 G or LN229 cells treated with linc00339 plasmid, Avasimibe (7.5 μM for 48 h) alone or in combination with linc00339 plasmids.

    View All Acyltransferase Isoform Specific Products:

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    ACAT1 ACAT2 MGAT2 ACAT

    • Biological Activity

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    • References

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    Description

    Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively[1]. Avasimibe can be used for the research of prostate cancer[2].

    IC50 & Target[1]

    ACAT1

    24 μM (IC50)

    ACAT2

    9.2 μM (IC50)

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Avasimibe Related Antibodies

    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.
    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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.
    Molecular Weight

    501.72

    Appearance

    Solid

    Formula

    C29H43NO4S
    CAS No.
    SMILES

    O=C(NS(=O)(OC1=C(C(C)C)C=CC=C1C(C)C)=O)CC2=C(C(C)C)C=C(C(C)C)C=C2C(C)C
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (199.31 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 7.5 mg/mL (14.95 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 7.5 mg/mL (14.95 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: 7.5 mg/mL (14.95 mM); Clear solution; Need ultrasonic

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.50%

    COA (249 KB) LCMS (256 KB)

    Handling Instructions (2659 KB)
    References
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    Avasimibe Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    Avasimibe166518-60-1CI-1011 PD-148515CI1011CI 1011PD148515PD 148515PD-148515AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseorallyactiveACATSOATACAT1ACAT2Inhibitorinhibitorinhibit

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