1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. CYP19A1/CYP11B2-IN-1

CYP19A1/CYP11B2-IN-1 (Compound X21) is a potent and selective aromatase and aldosterone synthase dual inhibitor with IC50s of 2.3 nM and 29 nM for aromatase (CYP19A1) and aldosterone synthase (CYP11B2), respectively. CYP19A1/CYP11B2-IN-1 has excellent antiproliferative and pro-apoptotic activity against the cancer cell. CYP19A1/CYP11B2-IN-1 can be used for research of breast cancer.

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

CYP19A1/CYP11B2-IN-1 Chemical Structure

CYP19A1/CYP11B2-IN-1 Chemical Structure

CAS No. : 183500-36-9

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Description

CYP19A1/CYP11B2-IN-1 (Compound X21) is a potent and selective aromatase and aldosterone synthase dual inhibitor with IC50s of 2.3 nM and 29 nM for aromatase (CYP19A1) and aldosterone synthase (CYP11B2), respectively. CYP19A1/CYP11B2-IN-1 has excellent antiproliferative and pro-apoptotic activity against the cancer cell. CYP19A1/CYP11B2-IN-1 can be used for research of breast cancer[1].

In Vitro

CYP19A1/CYP11B2-IN-1 (Compound X21) (0.001-100 μM, 24 h) shows a time- and concentration-dependent proliferation inhibition on MCF-7 and MDA-MB-231 cells[1].
CYP19A1/CYP11B2-IN-1 (700 nM, 24 h) significantly inhibits the phosphorylation of mTOR in MCF-7 cells, thereby negatively modulating the PI3K/Akt/mTOR axis[1].
CYP19A1/CYP11B2-IN-1 (20-30 μM) has no significant inhibition of hERG and Nav1.5, indicating no toxicity to the heart[1].

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

Cell Proliferation Assay[1]

Cell Line: MCF-7 and MDA-MB-231 cells
Concentration: 0.001-100 μM
Incubation Time: 24-72 h
Result: Inhibited the MCF-7 cells proliferation with an IC50 of 0.26±0.03 μM.
Inhibited the MDA-MB-231 cells proliferation with an IC50 of 27.10 ± 5.15 μM.
Confirmed no toxicity on normal cells.

Apoptosis Analysis[1]

Cell Line: MCF-7 and MDA-MB-231 cells
Concentration: 0.35-1 μM, 10-50 μM
Incubation Time: 24 h
Result: Increase in the extent of DNA fragmentation.
Increased the apoptotic signal in MDA-MB-231 cells with higher concentrations (> 40 μM).
Molecular Weight

213.24

Formula

C12H11N3O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=CC=C(CN2C=NC=C2CO)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (586.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.6896 mL 23.4478 mL 46.8955 mL
5 mM 0.9379 mL 4.6896 mL 9.3791 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.6896 mL 23.4478 mL 46.8955 mL 117.2388 mL
5 mM 0.9379 mL 4.6896 mL 9.3791 mL 23.4478 mL
10 mM 0.4690 mL 2.3448 mL 4.6896 mL 11.7239 mL
15 mM 0.3126 mL 1.5632 mL 3.1264 mL 7.8159 mL
20 mM 0.2345 mL 1.1724 mL 2.3448 mL 5.8619 mL
25 mM 0.1876 mL 0.9379 mL 1.8758 mL 4.6896 mL
30 mM 0.1563 mL 0.7816 mL 1.5632 mL 3.9080 mL
40 mM 0.1172 mL 0.5862 mL 1.1724 mL 2.9310 mL
50 mM 0.0938 mL 0.4690 mL 0.9379 mL 2.3448 mL
60 mM 0.0782 mL 0.3908 mL 0.7816 mL 1.9540 mL
80 mM 0.0586 mL 0.2931 mL 0.5862 mL 1.4655 mL
100 mM 0.0469 mL 0.2345 mL 0.4690 mL 1.1724 mL
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CYP19A1/CYP11B2-IN-1 Related Classifications

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  • 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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Product Name:
CYP19A1/CYP11B2-IN-1
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