Biological Activity
Orally active, potent aromatase (CYP19) inhibitor (IC50 values are 0.4 and 0.12 nM at rat ovary and human placenta cells respectively) that only weakly inhibits the synthesis of other steroid hormones. Reduces plasma estrogen levels into ranges induced by ovariectomy and inhibits testosterone-induced breast cancer cell growth in vitro (IC50 = 0.13 nM).
Licensing Information
(Sold with the permission of Astellas Pharma Inc.)
Technical Data
| M. Wt | 354.2 |
| Formula | C16H12BrN5 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 148869-05-0 |
| PubChem ID | 177865 |
| InChI Key | GGPPBTSXFROGAE-UHFFFAOYSA-N |
| Smiles | BrC(C=C3)=CC=C3CN(N2C=NN=C2)C1=CC=C(C#N)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 35.42 | 100 | |
| ethanol | 8.86 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 354.2. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.82 mL | 14.12 mL | 28.23 mL |
| 5 mM | 0.56 mL | 2.82 mL | 5.65 mL |
| 10 mM | 0.28 mL | 1.41 mL | 2.82 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Okada et al (1996) Studies on aromatase inhibitors I. Synthesis and biological evaulation of 4-amino-4H-1,2,4-triaole derivatives. Chem.Pharm.Bull. 44 1871 PMID: 8904814
Kudoh et al (1995) The potent and selective inhibiton of estrogen production by non-steroidal aromatase inhibitor, YM511. J.Steroid Biochem.Molec.Biol. 54 265 PMID:
Kudoh et al (1996) Inhibitory effect of a novel non-steroidal aromatase inhibitor, YM511 on the proliferation of MCF-7 human breast cancer cell. J.Steroid Biochem.Molec.Biol. 58 189 PMID:
Keywords: YM 511, supplier, Potent, aromatase, CYP19, inhibitors, inhibits, Cytochrome, P450, ERR, Estrogen, Receptors, YM511, Cytochrome, P450, Estrogen, and, Related, Receptors, Cytochrome, P450, Tocris Bioscience
Tocris Bioscience是一家专卖生命科学研究chemicals, peptides and antibodies的知名品牌，其产品也广为各大药厂、大学、研究机构，超过五万名科学研究者所采用。 目前，產品內容已超過一千六百種以上，並每年持續不斷的增加新的產品。目前，产品内容已超过一千六百种以上，并每年持续不断的增加新的产品。
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