Biological Activity
Estrogen receptor antagonist/partial agonist. Selective and potent inhibitor of mammalian sterol isomerase. Neuroprotective in female rats in vivo. Also high affinity agonist at the membrane estrogen receptor GPER. Tamoxifen (Cat.No. 6432) is also available.
Licensing Information
Sold with the permission of AstraZeneca UK Ltd.
Compound Libraries
Tamoxifen citrate is also offered as part of the Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 563.65 |
| Formula | C26H29NO.C6H8O7 |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 54965-24-1 |
| PubChem ID | 2733525 |
| InChI Key | FQZYTYWMLGAPFJ-OQKDUQJOSA-N |
| Smiles | CC/C(C2=CC=CC=C2)=C(C3=CC=CC=C3)/C1=CC=C(OCCN(C)C)C=C1.O=C(O)CC(O)(C(O)=O)CC(O)=O |
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 | 56.37 | 100 | |
| ethanol | 2.82 | 5mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 563.65. 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 | 1.77 mL | 8.87 mL | 17.74 mL |
| 5 mM | 0.35 mL | 1.77 mL | 3.55 mL |
| 10 mM | 0.18 mL | 0.89 mL | 1.77 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.35 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Wakeling et al (1984) Non-steroidal anti-estrogens - receptor binding and biological response in rat uterus, rat mammary carcinoma and human breast cancer cells. J.Steroid.Biochem. 20 111 PMID: 6538611
Mehta et al (2003) Tamoxifen, a selective estrogen receptor modulator, reduces ischemic damage caused by middle cerebral artery occlusion in the ovariectomized female rat. Neuroendocrinology 77 44 PMID: 12624540
Thomas et al (2005) Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells. Endocrinology 146 624 PMID: 15539556
Merck Index 12 9216 PMID:
Paul et al (1998) Both the immunosuppressant SR31747 and the antioestrogen tamoxifen bind to an emopamil-insensitive site of mammalian Δ8-Δ7 sterol isomerase. J.Pharmacol.Exp.Ther. 285 1302 PMID: 9618436
Todorova et al (2011) Tamoxifen and raloxifene suppress the proliferation of estrogen receptor-negative cells through inhibition of glutamine uptake. Cancer Chemother. Pharmacol. 67 285 PMID: 20383709
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