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).


Price and Availability

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Price

10mg
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100mg
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1g
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25mg
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200mg
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2g
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50mg
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500mg
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5g
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GTX-758 is not in stock, but is available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

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.