product name Toremifene Citrate
Description: Toremifene Citrate (NSC 613680) is an orally available and selective estrogen receptor modulator (SERM), it is used in the treatment of advanced breast cancer. Toremifene citrate acts by antagonizing the actions of estrogen in the body. Toremifene (7.5 mM) causes approximately 60% of the cells to exhibit morphologic characteristics typical of cells undergoing programmed death, or apoptosis in human breast cancer cells. Toremifene (5-10 mM) results in elevated levels of TRPM-2 and TGF beta 1 mRNAs in in vitro or in vivo grown tumor cells.
References: J Natl Cancer Inst. 1993 Sep 1;85(17):1412-8; Carcinogenesis. 1995 Nov;16(11):2733-41.
598.08
Formula
C32H36ClNO8
CAS No.
89778-27-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (167.2 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
NSC 613680
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/1941756
| In Vitro |
In vitro activity: Toremifene (7.5 mM) causes approximately 60% of the cells to exhibit morphologic characteristics typical of cells undergoing programmed death, or apoptosis in human breast cancer cells. Toremifene (5-10 mM) results in elevated levels of TRPM-2 and TGF beta 1 mRNAs in in vitro or in vivo grown tumor cells. Toremifene causes growth inhibition of estrogen-sensitive breast cancer cells by inducing some cells to undergo apoptosis and by inhibiting other cells from entering mitosis. Toremifene induces a dose-dependent level of adducts that is lower than that observed for TAM. Toremifene significantly enhances endogenous DNA adduct formation. Toremifene affects the cell turnover by inhibiting mitotic activity and modifying abundant spontaneous apoptosis in DMBA-induced rat mammary carcinoma. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Toremifene, at the highest tested dose, increases the incidence of hepatocellular carcinomas in the DEN-initiated groups to a level one-third that observed with Tamoxifen administration to DEN-initiated rats. Toremifene increases the incidence of hypernephromas in previously DEN-initiated rats. Toremifene results in aneuploidy in 50% of the cells examined and compared with the 85% level induced by Tamoxifen in female Sprague-Dawley rats. |
| Animal model | |
| Formulation & Dosage | |
| References | J Natl Cancer Inst. 1993 Sep 1;85(17):1412-8; Carcinogenesis. 1995 Nov;16(11):2733-41. |
