GTX-758, also known as Capesaris, is a n orally available, nonsteroidal selective estrogen receptor (ER) alpha agonist with potential antineoplastic activity. Upon administration of GTx-758, this agent suppresses the secretion of the gonadotropins follicle-stimulating hormone (FSH) and luteinizing hormone (LH) by the pituitary gland through feedback inhibition. In males, the inhibition of LH secretion prevents the synthesis of androgens, including testosterone, by the testes. This may result in suppressed total serum testosterone to the levels observed in castration. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

MedKoo Cat#: 201453 Name: GTX-758 CAS#: 938067-78-8 Chemical Formula: C19H13F2NO3 Exact Mass: 341.08635 Molecular Weight: 341.30823 Elemental Analysis: C, 66.86; H, 3.84; F, 11.13; N, 4.10; O, 14.06

Synonym: GTX758; GTX-758; GTX 758; Capesaris.

IUPAC/Chemical Name: 3-fluoro-N-(4-fluorophenyl)-4-hydroxy-N-(4-hydroxyphenyl)benzamide.

InChi Key: FBCQEUMZZNVQKD-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H13F2NO3/c20-13-2-4-14(5-3-13)22(15-6-8-16(23)9-7-15)19(25)12-1-10-18(24)17(21)11-12/h1-11,23-24H

SMILES Code: O=C(N(C1=CC=C(F)C=C1)C2=CC=C(O)C=C2)C3=CC=C(O)C(F)=C3

Technical Data

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

References

1: Fenner A. Prostate cancer: GTx-758 reduces testosterone. Nat Rev Urol. 2014 Aug;11(8):422. doi: 10.1038/nrurol.2014.165. Epub 2014 Jul 8. PubMed PMID: 25002202.

2: Yu EY, Getzenberg RH, Coss CC, Gittelman MM, Keane T, Tutrone R, Belkoff L, Given R, Bass J, Chu F, Gambla M, Gaylis F, Bailen J, Hancock ML, Smith J, Dalton JT, Steiner MS. Selective Estrogen Receptor Alpha Agonist GTx-758 Decreases Testosterone with Reduced Side Effects of Androgen Deprivation Therapy in Men with Advanced Prostate Cancer. Eur Urol. 2014 Jun 24. pii: S0302-2838(14)00532-6. doi: 10.1016/j.eururo.2014.06.011. [Epub ahead of print] PubMed PMID: 24968970.

3: Coss CC, Jones A, Parke DN, Narayanan R, Barrett CM, Kearbey JD, Veverka KA, Miller DD, Morton RA, Steiner MS, Dalton JT. Preclinical characterization of a novel diphenyl benzamide selective ERα agonist for hormone therapy in prostate cancer. Endocrinology. 2012 Mar;153(3):1070-81. doi: 10.1210/en.2011-1608. Epub 2012 Jan 31. PubMed PMID: 22294742.