Degarelix acetate
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MedKoo CAT#: 100255

CAS#: 934246-14-7 (acetate)

Description: Degarelix, also known as FE-200486 and ASP-3550, is a long-acting, synthetic peptide with gonadotrophin-releasing hormone (GnRH) antagonistic properties. Degarelix targets and blocks GnRH receptors located on the surfaces of gonadotroph cells in the anterior pituitary, thereby reducing secretion of luteinizing hormone (LH) by pituitary gonadotroph cells and so decreasing testosterone production by interstitial (Leydig) cells in the testes. Degarelix acetate was approved in 2008.


Price and Availability

Size Price Shipping out time Quantity
10mg USD 190 Same day
25mg USD 350 Same day
50mg USD 550 Same day
100mg USD 950 Same day
200mg USD 1650 Same day
500mg USD 2950 Same day
1g USD 3850 Same day
2g USD 7450 2 Weeks
5g USD 15650 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-31. Prices are subject to change without notice.

Degarelix acetate, purity > 98%, is in stock. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 100255
Name: Degarelix acetate
CAS#: 934246-14-7 (acetate)
Chemical Formula: C84H107ClN18O18
Exact Mass:
Molecular Weight: 1692.31
Elemental Analysis: C, 60.34; H, 6.36; Cl, 2.17; N, 15.45; O, 15.68


Related CAS #: 214766-78-6 (free base)   934246-14-7 (acetate)    

Synonym: FE200486; FE-200486; FE 200486; ASP3550; ASP-3550; ASP 3550. Degarelix acetate; tradename Firmagon.

IUPAC/Chemical Name: (S)-N-(4-((2S,5S,8R,11R,14R)-2-(((R)-1-(((S)-1-(((S)-1-((S)-2-(((R)-1-amino-1-oxopropan-2-yl)carbamoyl)pyrrolidin-1-yl)-6-(isopropylamino)-1-oxohexan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)amino)-1-oxo-3-(4-ureidophenyl)propan-2-yl)carbamoyl)-11-(4-chlorobenzyl)-5-(hydroxymethyl)-14-(naphthalen-2-ylmethyl)-4,7,10,13,16-pentaoxo-8-(pyridin-3-ylmethyl)-3,6,9,12,15-pentaazaheptadecyl)phenyl)-2,6-dioxohexahydropyrimidine-4-carboxamide.

InChi Key: AUTFSFUMNFDPLH-KYMMNHPFSA-N

InChi Code: (S)-N-(4-((2S,5S,8R,11R,14R)-2-(((R)-1-(((S)-1-(((S)-1-((S)-2-(((R)-1-amino-1-oxopropan-2-yl)carbamoyl)pyrrolidin-1-yl)-6-(isopropylamino)-1-oxohexan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)amino)-1-oxo-3-(4-ureidophenyl)propan-2-yl)carbamoyl)-11-(4-chlorobenzyl)-5-(hydroxymethyl)-14-(naphthalen-2-ylmethyl)-4,7,10,13,16-pentaoxo-8-(pyridin-3-ylmethyl)-3,6,9,12,15-pentaazaheptadecyl)phenyl)-2,6-dioxohexahydropyrimidine-4-carboxamide acetate

SMILES Code: O=C([C@H](CC(N1)=O)NC1=O)NC2=CC=C(C[C@@H](C(N[C@H](CC3=CC=C(NC(N)=O)C=C3)C(N[C@@H](CC(C)C)C(N[C@@H](CCCCNC(C)C)C(N4[C@H](C(N[C@H](C)C(N)=O)=O)CCC4)=O)=O)=O)=O)NC([C@H](CO)NC([C@@H](CC5=CC=CN=C5)NC([C@@H](CC6=CC=C(Cl)C=C6)NC([C@@H](CC7=CC=C8C=CC=CC8=C7)NC(C)=O)=O)=O)=O)=O)C=C2.CC(O)=O


Technical Data

Appearance:
White to off-white solid powder

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

Certificate of Analysis:

Safety Data Sheet (SDS):

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


Additional Information

Related CAS#
214766-78-6 (Degarelix );
934246-14-7 (Degarelix acetate)


References

1: Sofikerim M. Re: Crawford et al.: Long-term Tolerability and Efficacy of Degarelix: 5-Year Results From a Phase III Extension Trial With a 1-Arm Crossover From Leuprolide to Degarelix (Urology 2014;83:1122-1128). Urology. 2014 Nov;84(5):1250. doi: 10.1016/j.urology.2014.07.053. Epub 2014 Oct 24. PubMed PMID: 25443943.

2: Maeda T, Kosaka T, Honda A, Okata U, Hayakawa N, Ito Y, Nagata H, Chen KR, Nakamura S, Oya M. Evaluation of histopathological findings at the injection site following degarelix administration. Support Care Cancer. 2014 Oct 31. [Epub ahead of print] PubMed PMID: 25358643.

3: Lee D, Nielsen SK, van Keep M, Andersson F, Greene D. Quality of Life Improvement in Patients Treated with Degarelix versus Leuprorelin for Advanced Prostate Cancer. J Urol. 2014 Sep 28. pii: S0022-5347(14)04572-8. doi: 10.1016/j.juro.2014.09.098. [Epub ahead of print] PubMed PMID: 25264336.

4: Boccon-Gibod L, Albers P, Morote J, van Poppel H, de la Rosette J, Villers A, Malmberg A, Neijber A, Montorsi F. Degarelix as an intermittent androgen deprivation therapy for one or more treatment cycles in patients with prostate cancer. Eur Urol. 2014 Oct;66(4):655-63. doi: 10.1016/j.eururo.2014.05.037. Epub 2014 Jun 18. PubMed PMID: 24954791.

5: Carter NJ, Keam SJ. Degarelix: a review of its use in patients with prostate cancer. Drugs. 2014 Apr;74(6):699-712. doi: 10.1007/s40265-014-0211-y. PubMed PMID: 24756432.

6: Crawford ED, Shore ND, Moul JW, Tombal B, Schröder FH, Miller K, Boccon-Gibod L, Malmberg A, Olesen TK, Persson BE, Klotz L. Long-term tolerability and efficacy of degarelix: 5-year results from a phase III extension trial with a 1-arm crossover from leuprolide to degarelix. Urology. 2014 May;83(5):1122-8. doi: 10.1016/j.urology.2014.01.013. Epub 2014 Mar 22. PubMed PMID: 24661333.

7: Cui Y, Zong H, Yan H, Li N, Zhang Y. Degarelix versus goserelin plus bicalutamide therapy for lower urinary tract symptom relief, prostate volume reduction and quality of life improvement in men with prostate cancer: a systematic review and meta-analysis. Urol Int. 2014;93(2):152-9. doi: 10.1159/000356272. Epub 2014 Mar 1. PubMed PMID: 24603064.

8: Lee D, Porter J, Gladwell D, Brereton N, Nielsen SK. A cost-utility analysis of degarelix in the treatment of advanced hormone-dependent prostate cancer in the United Kingdom. J Med Econ. 2014 Apr;17(4):233-47. doi: 10.3111/13696998.2014.893240. Epub 2014 Feb 25. PubMed PMID: 24568188.

9: Clyne M. Tipping the balance in favour of degarelix for ADT. Nat Rev Urol. 2014 Feb;11(2):67. doi: 10.1038/nrurol.2014.11. Epub 2014 Jan 28. PubMed PMID: 24473414.

10: Klotz L, Miller K, Crawford ED, Shore N, Tombal B, Karup C, Malmberg A, Persson BE. Disease Control Outcomes from Analysis of Pooled Individual Patient Data from Five Comparative Randomised Clinical Trials of Degarelix Versus Luteinising Hormone-releasing Hormone Agonists. Eur Urol. 2014 Dec;66(6):1101-8. doi: 10.1016/j.eururo.2013.12.063. Epub 2014 Jan 9. PubMed PMID: 24440304.