1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. Aromatase-IN-8

Aromatase-IN-8 is a selective Aromatase inhibitor against an IC50 of 0.05 µM. Aromatase-IN-8 exhibits selective antiproliferative effects against estrogen receptor-positive breast cancer cell lines, while showing no toxicity toward non-tumoral cells. Aromatase-IN-8 suppresses estrogen active, increases testosterone levels, and downregulates estrogen receptor expression and phosphorylation. Aromatase-IN-8 can be used for triple negative breast cancer research.

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Aromatase-IN-8

Aromatase-IN-8 Chemical Structure

CAS No. : 1244904-19-5

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Description

Aromatase-IN-8 is a selective Aromatase inhibitor against an IC50 of 0.05 µM. Aromatase-IN-8 exhibits selective antiproliferative effects against estrogen receptor-positive breast cancer cell lines, while showing no toxicity toward non-tumoral cells. Aromatase-IN-8 suppresses estrogen active, increases testosterone levels, and downregulates estrogen receptor expression and phosphorylation. Aromatase-IN-8 can be used for triple negative breast cancer research[1].

IC50 & Target[1]

Aromatase

0.05 μM (IC50)

In Vitro

Aromatase-IN-8 (compound 17) (72 h) displays prominent anticancer effects in ER + breast cancer cell lines (T47D and MCF-7 cells) and triple-negative breast cancer cell line (MDA-231 cells) with IC50 = 42.90, 79.43 and > 100 µM[1].
Aromatase-IN-8 (6.25-100 µM, 24 and 72 h) reduces cell viability effects correlate with increasing dosage in MCF-7 cells and MDA-MB-231 cells[1].
Aromatase-IN-8 (0-50 μM, 24 h) reduces ERα and ERβ protein levels in MCF-7 cells[1].
Aromatase-IN-8 (6.25-50 μM, 8 h) reveals low 17β-estradiol and estrone small suppressive effects on estrogen synthesis leads to a more abundant accumulation of testosterone at concentrations above 12.5 µM in MCF-7 cells[1].
Aromatase-IN-8 downregulates fatty acid degradation, upregulates pantothenate and CoA biosynthesis, valine and sphingosine accumulation and has the strong anticancer effects at higher doses in MCF-7 cells[1].

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

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 12.5, 25 and 50 μM
Incubation Time: 24 h
Result: Reduced the expression of both non-phosphorylated and phosphorylated Erα and Erβin a dose-dependent manner.
Molecular Weight

346.88

Formula

C17H19ClN4S

CAS No.
SMILES

CC1=NN(C(Cl)=C1CN(CC2=CSC=C2)CC3=CN=CC=C3)C

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Aromatase-IN-8
Cat. No.:
HY-180535
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