Toremifene Citrate (NK 622)

Catalog No.S1776 Batch:S177602

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Technical Data

Formula

C32H36ClNO8
Molecular Weight 598.08 CAS No. 89778-27-8
Solubility (25°C)* In vitro DMSO 100 mg/mL (167.2 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Toremifene Citrate (NK 622, NSC 613680) is an oral selective estrogen receptor modulator (SERM), used in the treatment of advanced breast cancer.
Targets
Estrogen receptor [1]
In vitro 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. [1] Toremifene induces a dose-dependent level of adducts that is lower than that observed for TAM. Toremifene significantly enhances endogenous DNA adduct formation. [2] Toremifene affects the cell turnover by inhibiting mitotic activity and modifying abundant spontaneous apoptosis in DMBA-induced rat mammary carcinoma. [3]
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. [4] Toremifene results in aneuploidy in 50% of the cells examined and compared with the 85% level induced by Tamoxifen in female Sprague-Dawley rats. [5]

Protocol (from reference)

Customer Product Validation

Data from [Data independently produced by , , Nature, 2018, 560(7718):372-376]

Data from [Data independently produced by , , J Biomed Res, 2016, 30(5): 393-410.]

Selleck's Toremifene Citrate (NK 622) has been cited by 8 publications

Hormonally Regulated Myogenic miR-486 Influences Sex-specific Differences in Cancer-induced Skeletal Muscle Defects [ Endocrinology, 2021, 162(10)bqab142] PubMed: 34265069
Reversal of Infected Host Gene Expression Identifies Repurposed Drug Candidates for COVID-19 [ bioRxiv, 2020, 2020/9/20.4.7.30734] PubMed: 32511305
Arbidol and Other Low-Molecular-Weight Drugs That Inhibit Lassa and Ebola Viruses. [ J Virol, 2019, 93(8)] PubMed: 30700611
Inhibition of Ebola Virus by a Molecularly Engineered Banana Lectin. [ PLoS Negl Trop Dis, 2019, 13(7):e0007595] PubMed: 31356611
Accumulation of 8,9-unsaturated sterols drives oligodendrocyte formation and remyelination [Hubler Z, et al. Nature, 2018, 560(7718):372-376] PubMed: 30046109
Comparative analysis of media effects on human induced pluripotent stem cell-derived cardiomyocytes in proarrhythmia risk assessment [ J Pharmacol Toxicol Methods, 2017, 90:39-47] PubMed: 29155283
New insights into estrogenic regulation of O6-methylguanine DNA-methyltransferase (MGMT) in human breast cancer cells: Co-degradation of ER-α and MGMT proteins by fulvestrant or O6-benzylguanine indicates fresh avenues for therapy. [Paranjpe A, et al. J Biomed Res, 2016, 30(5):393-410] PubMed: 27845303
Combining genomic and network characteristics for extended capability in predicting synergistic drugs for cancer. [ Nat Commun, 2015, 6:8481] PubMed: 26412466

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.