Toremifene

SKU: orb1223722

Description

Toremifene (NK 622; FC 1157a) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis.(In Vitro):Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis and other adverse effects resulting from ADT with prostate cancer.The growth of Ac-1 cells was inhibited by tamoxifen, toremifene and atamestane in vitro with IC50values of 1.8±1.3μM, 1±0.3μM and 60.4±17.2μM, respectively. The combination of toremifene plusatamestane was found to be better than toremifene or atamestane alone in vitro.(In Vivo):The effect of this combination was then studied in vivo using Ac-1 xenografts grown in ovariectomized female SCID mice. The mice were injected with toremifene (1000μg/day), atamestane (1000μg/day), tamoxifen (100μg/day), or the combination of toremifene plus atamestane. In this study, our results indicate that the combination of toremifene plus atamestane was as effective as toremifene or tamoxifen alone but may not provide any additional benefit over toremifene alone or tamoxifen alone.

Key Properties

• CAS Number: 89778-26-7
• MW: 405.96
• Purity: >98% (HPLC)
• Formula: C₂₆H₂₈ClNO
• SMILES: CN(C)CCOC1=CC=C(C=C1)/C(=C(/CCCl)\C2=CC=CC=C2)/C3=CC=CC=C3
• Target: Estrogen Receptor/ERR
• Solubility: Soluble in DMSO

Bioactivity

• In Vivo:
  The effect of this combination was then studied In vivo using Ac-1 xenografts grown in ovariectomized female SCID mice. The mice were injected with toremifene (1000μg/day), atamestane (1000μg/day), tamoxifen (100μg/day), or the combination of toremifene plus atamestane. In this study, our results indicate that the combination of toremifene plus atamestane was as effective as toremifene or tamoxifen alone but may not provide any additional benefit over toremifene alone or tamoxifen alone.
• In Vitro:
  Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis and other adverse effects resulting from ADT with prostate cancer. The growth of Ac-1 cells was inhibited by tamoxifen, toremifene and atamestane in vitro with IC50values of 1.8±1.3 μM, 1±0.3 μM and 60.4±17.2 μM, respectively. The combination of toremifene plusatamestane was found to be better than toremifene or atamestane alone in vitro.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NK 622 | FC 1157a

Quick Database Links

Gene Symbol

Estrogen Receptor/ERR