Name: Toremifene Citrate
Synonyms: Toremifene Citrate;FC 1157A; Fareston; NK 622; NSC 613680
CAS: 89778-27-8
Molecular Formula: C26H28ClNO. C6H8O7
Molecular Weight: 598.09
Melting Point: 158-164 º C
Boiling Point: 535.1 º C at 760 mmHg
Density: 1.045g/cm3
Refractive index: 1, 416-1, 418
Appearance: White or almost white powder
Assay:99%
Standard:USP
Export Markets:Global
Package: 1kg/foil bag; 25kg/drum
Delivery time: Within 18 hours upon receipt of payment
Delivery: EMS, DHL, TNT, FedEx, UPS
Usage:Originally developed to fight breast cancer, bodybuilders have used Fareston to successfully fight gynocomastia caused when testosterone converts to estrogen in the body and men grow breasts. This substance can be used for little else and other similar compounds, such as Nolvadex or Clomid, are much more effective in post-cycle-therapy. Other drugs in same class: Tamoxifen citrate..
1. Quick Detail:
1. CAS No:89778-27-8
2. Molecular Formula: C26H28ClNO.C6H8O7
3. Assay: 97.0%~103.0%
4. Appearance: White crystalline powder.
5. Usage:Originally developed to fight breast cancer, bodybuilders have used Fareston to successfully fight gynocomastia caused when converts to estrogen in the body and men grow breasts. This substance can be used for little else and other similar compounds, such as Nolvade or Clomid, are much more effective in post-cycle-therapy.
2. Description:
Toremifen(e) citrate, chemical name Z-2-[4-(4-chloro-1, 2-diphenyl)-1-butenyl]phenoxy]-N, N -Dimethyl ethylamine monophthalate, a new generation of anti-estrogen antitumor drug developed by Farmos in Finland in 1979. It is a derivative of non-steroidal tristyryl. It was first developed in Finland in 1988. The listed non-steroidal anti-estrogen antitumor drugs are mainly used for the treatment of breast cancer.
is a member of a category, family, and class of drugs that are known as SERMs (Selective Estrogen Receptor Modulators). SERMs fall under an even broader category of drugs that are known as anti-estrogens, and the cousin family of SERMs (that also fall under anti-estrogens) are aromatase inhibitors, commonly abbreviated as AIs. SERMs include compounds such as Nolvade and Clomid (Clomiphene Citrate). Aromatase inhibitors (AIs) include compounds such as Arimide ) Aromasin, (Femara). Although the two fall under the category of anti-estrogens, they are both sub-categories that branch off into their own families, as SERMs and AIs differ greatly in their mechanism of action within the human body concerning how they control or block Estrogen. There has been much misunderstanding and misconception in previous decades as to what each of these do, and this should always be first clarified to the reader before describing Toremifen.
3. Applications:
Toremifen citrate is an oral selective estrogen receptor modulator (SERM) which helps oppose the actions of estrogen in the body. Licensed in the United States under the brand name Fareston, toremifen citrate is FDA-approved for use in advanced (metastatic) breast cancer. It is also being evaluated for prevention of prostate cancer under the brand name Acapodene.
It has already been covered that Toremifen is a SERM, and serves to block Estrogen at various receptor sites in certain tissues within the body (breast tissue in particular). As a layman explanation, Toremifen pretends to be a 'fake' Estrogen that occupies Estrogen receptors within breast tissue. With these receptors occupied by Toremifen, real Estrogen cannot perform their jobs there.
Toremifen does not reduce total blood plasma levels of Estrogen. In addition to being antagonistic to Estrogen receptors in breast tissue, it is also antagonistic to Estrogen at the hypothalamus gland (this essentially 'tricks' the hypothalamus into thinking there is little or no circulating Estrogen levels in the body, causing it to increase its manufacture of so that it can utilize aromatization to restore these levels.
Toremifen is also agonistic to Estrogen receptors in other tissues in the body (within the liver in particular). This means that whileToremifen will act as an anti-estrogen in breast tissue and the hypothalamus, it will act as an Estrogen within the liver. This can have beneficial impacts especially during an cycle, such as improving and shifting cholesterol levels into a more favorable range.
4. Specification:
COA:
Test items Quality requirements Results
Description White or like white crystalline powder White crystalline powder
Solubility Freely soluble in pyridine and acetic acid(100), sparingly soluble in methanol, slightly soluble in ethanol, very slightly soluble in water, and practically insoluble in diethyl ether Freely soluble in pyridine and acetic acid(100), sparingly soluble in methanol, slightly soluble in ethanol, very slightly soluble in water, and practically insoluble in diethyl ether
Melting point 159~163ºC 159.0~160.5ºC
Identification
(a)Positive reaction Must comply Complies
(b)Positive reaction Must comply Complies
(c) UV There is the strongest absorption at the wavelength of 234~238nm and 275~278nm. There is the strongest absorption at the wavelength of 236.8nm and 276.2nm.
(d) IR There is absorption at 1741, 1703, 1585, 1241 and 706cm-1 . There is absorption at 1741, 1703, 1585, 1241 and 706cm-1 .
Purity 99%
(a) Relative substances
E-isomer ≤0.5% 0.001%
Total relative substances ≤1.0% 01%
(b)Heavy metals ≤10ppm <10ppm
Loss on drying ≤1.0% 0.1%
≤0.089% 0.0002%
Ethanol ≤0.5% 0
Acetone ≤0.5% 0.21%
≤0.072% 0.0001%
Chlorobenzen ≤0.036% 0
Benzene ≤0.0002% 0
Residue on ignition ≤0.1% 0.04%
Assay ≥98.5% (Calculated by C26H28ClNO .C6H8O7) 99.7%
Conclusion: The results comply with the requirements of the export standard.
Toremifen(e) citrate Pharmacological effects:
The combination of toremifen(e) citrate with estrogen receptors can produce estrogen-like or anti-estrogen effects, or both, depending on the length of treatment, animal species, sex, and target organ. In general, non-steroidal tristyryl derivatives act primarily as anti-estrogen in humans and rats and as estrogen-like effects in mice. The use of toremifen(e) in postmenopausal breast cancer patients induced a moderate decrease in serum total cholesterol and low density lipoprotein (LDL). Toremifen(e) citrate and estrogen competitively bind to estrogen receptors in cytoplasm of breast cancer cells, preventing estrogen-induced DNA synthesis and proliferation in cancer cells. A large dose of toremifen(e) citrate was used in some experimental tumors, demonstrating the non-estrogen-dependent antitumor effects of toremifen(e) citrate. The anti-breast cancer effect of toremifen(e) citrate is mainly an anti-estrogen effect, and may also have other anti-cancer mechanisms (change in tumor gene expression, secrete growth factors, induce apoptosis, and affect cell cycle dynamics).