GTX-758

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 201453

CAS#: 938067-78-8

Description: 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).

Chemical Structure

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GTX-758
CAS# 938067-78-8
Instruction

Theoretical Analysis

MedKoo Cat#: 201453
Name: GTX-758
CAS#: 938067-78-8
Chemical Formula: C19H13F2NO3
Exact Mass: 341.09
Molecular Weight: 341.308
Elemental Analysis: C, 66.86; H, 3.84; F, 11.13; N, 4.10; O, 14.06

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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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

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).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 341.31 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.