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Chemical Structure| 166518-60-1 Chemical Structure| 166518-60-1

Structure of Avasimibe
CAS No.: 166518-60-1

Chemical Structure| 166518-60-1

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Avasimibe is an ACAT inhibitor with IC50 of 3.3 μM, it also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9/13.9 and 26.5 μM, respectively.

Synonyms: CI-1011; PD-148515; Cl-1011

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Product Details of Avasimibe

CAS No. :166518-60-1
Formula : C29H43NO4S
M.W : 501.72
SMILES Code : 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
Synonyms :
CI-1011; PD-148515; Cl-1011
MDL No. :MFCD00934956
InChI Key :PTQXTEKSNBVPQJ-UHFFFAOYSA-N
Pubchem ID :166558

Safety of Avasimibe

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
B16F10 cells 1 μM 24, 48, or 72 h Enhanced cytotoxicity and proliferation of CD8+ T-cells were observed. PMC4851431
Various human cancer cells 5 µM 24 h Reduced cholesteryl ester storage, increased free cholesterol, led to apoptosis and inhibited proliferation. PMC5909415
glioblastoma cells 0 to 240 μM 24 or 48 h to determine the effect of avasimibe on cell proliferation, showing dose-dependent inhibition and increased apoptosis PMC7921416

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice B16F10 melanoma model Intragastric administration 15 mg/kg every 2 days Reduction in tumor size and improved survival rates were observed. PMC4851431
Mice PC3 and HCT116 tumor xenograft models Intravenous injection 75 mg/kg (7.5 mg/kg avasimibe) Daily for the first 5 days, followed by once every 4 days Suppressed tumor growth and extended length of survival time. PMC5909415
BALB/c-nu nude mice U87 xenograft model Intraperitoneal injection 15 or 30 mg/kg once per day for 18 days to assess the antitumor effect, showing significant tumor size and weight reduction PMC7921416

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.97mL

1.99mL

1.00mL

19.93mL

3.99mL

1.99mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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