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MedKoo Cat#: 527507 | Name: Proxalutamide
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Description:

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

Proxalutamide, also known as GT-0918, is an androgen receptor antagonist potentially for the treatment of metastatic castration-resistant prostate cancer (mCRPC). Proxalutamide protected against cell death in response to tumor necrosis factor alpha and interferon gamma.

Chemical Structure

Proxalutamide
Proxalutamide
CAS#1398046-21-3

Theoretical Analysis

MedKoo Cat#: 527507

Name: Proxalutamide

CAS#: 1398046-21-3

Chemical Formula: C24H19F4N5O2S

Exact Mass: 517.1196

Molecular Weight: 517.50

Elemental Analysis: C, 55.70; H, 3.70; F, 14.68; N, 13.53; O, 6.18; S, 6.20

Price and Availability

Size Price Availability Quantity
5mg USD 150.00 Ready to ship
10mg USD 250.00 Ready to ship
25mg USD 450.00 Ready to ship
50mg USD 750.00 Ready to ship
100mg USD 1,350.00 Ready to ship
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Related CAS #
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Synonym
Proxalutamide; Pruxelutamide; GT-0918; GT 0918; GT0918
IUPAC/Chemical Name
4-(4,4-dimethyl-3-(6-(3-(oxazol-2-yl)propyl)pyridin-3-yl)-5-oxo-2-thioxoimidazolidin-1-yl)-3-fluoro-2-(trifluoromethyl)benzonitrile
InChi Key
KCBJGVDOSBKVKP-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H19F4N5O2S/c1-23(2)21(34)32(17-9-6-14(12-29)19(20(17)25)24(26,27)28)22(36)33(23)16-8-7-15(31-13-16)4-3-5-18-30-10-11-35-18/h6-11,13H,3-5H2,1-2H3
SMILES Code
N#CC1=CC=C(N(C(N(C2=CC=C(CCCC3=NC=CO3)N=C2)C4(C)C)=S)C4=O)C(F)=C1C(F)(F)F
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
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

Preparing Stock Solutions

The following data is based on the product molecular weight 517.50 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
1: Zheng B, Zhao Q, Yang W, Feng P, Xin C, Ying Y, Yang B, Han B, Zhu J, Zhang M, Li G. Small-molecule antiviral treatments for COVID-19: A systematic review and network meta-analysis. Int J Antimicrob Agents. 2024 Mar;63(3):107096. doi: 10.1016/j.ijantimicag.2024.107096. Epub 2024 Jan 18. PMID: 38244811. 2: Qiao Y, Wotring JW, Zheng Y, Zhang CJ, Zhang Y, Jiang X, Pretto CD, Eyunni S, Parolia A, He T, Cheng C, Cao X, Wang R, Su F, Ellison SJ, Wang Y, Qin J, Yan H, Zhou Q, Ma L, Sexton JZ, Chinnaiyan AM. Proxalutamide reduces SARS-CoV-2 infection and associated inflammatory response. Proc Natl Acad Sci U S A. 2023 Jul 25;120(30):e2221809120. doi: 10.1073/pnas.2221809120. Epub 2023 Jul 17. PMID: 37459541; PMCID: PMC10372636. 3: Yang D, Ju M, Wang H, Jia Y, Wang X, Fang H, Fan J. Efficacy and safety of proxalutamide (GT0918) in severe or critically ill patients with COVID-19: study protocol for a prospective, open-label, single-arm, single-center exploratory trial. BMC Pharmacol Toxicol. 2023 Jun 15;24(1):38. doi: 10.1186/s40360-023-00678-7. PMID: 37322522; PMCID: PMC10268455. 4: Cheema HA, Rehman AU, Elrashedy AA, Mohsin A, Shahid A, Ehsan M, Ayyan M, Ismail H, Almas T. Antiandrogens for the treatment of COVID-19 patients: A meta- analysis of randomized controlled trials. J Med Virol. 2023 Apr;95(4):e28740. doi: 10.1002/jmv.28740. PMID: 37185842. 5: Yang DW, Ju MJ, Wang H, Jia YC, Wang XD, Fang H, Fan J. Proxalutamide for the treatment of COVID-19 rebound following Paxlovid treatment: Report of four cases and review of the literature. J Clin Lab Anal. 2023 Apr;37(7):e24880. doi: 10.1002/jcla.24880. Epub 2023 Apr 23. PMID: 37088868; PMCID: PMC10220290. 6: Zhou T, Qin S, Xu W, Tang S, Chen G, Li S, Hou J, Gao X, Shi G, Sun Z, Jin J, Chen L, Sun W, Liu B, Wang J, Meng Q, Wang D, Hu Z, He D, Yang Y, Song X, Fu C, Wang Y, Ye D, Zhang W. Proxalutamide in metastatic castration-resistant prostate cancer: Primary analysis of a multicenter, randomized, open-label, phase 2 trial. Int J Cancer. 2023 Aug 15;153(4):792-802. doi: 10.1002/ijc.34512. Epub 2023 Apr 10. PMID: 36919366. 7: Valencise FE, Palamim CVC, Marson FAL. Retraction of Clinical Trials about the SARS-CoV-2 Infection: An Unaddressed Problem and Its Possible Impact on Coronavirus Disease (COVID)-19 Treatment. Int J Environ Res Public Health. 2023 Jan 19;20(3):1835. doi: 10.3390/ijerph20031835. PMID: 36767202; PMCID: PMC9914919. 8: Jiang H, Ouyang Q, Yin Y, Tong Z, Shen K, Yuan Z, Geng C, Liu Y, Song G, Ran R, Li W, Qu Q, Wang M, Meng L, Tong Y, Li H. Proxalutamide in patients with AR- positive metastatic breast cancer: Results from an open-label multicentre phase Ib study and biomarker analysis. Eur J Cancer. 2022 Nov;176:1-12. doi: 10.1016/j.ejca.2022.08.025. Epub 2022 Sep 28. PMID: 36182805. 9: Frontiers Editorial Office. Retraction: Proxalutamide Reduces the Rate of Hospitalization for COVID-19 Male Outpatients: A Randomized Double-Blinded Placebo-Controlled Trial. Front Med (Lausanne). 2022 Jun 10;9:964099. doi: 10.3389/fmed.2022.964099. PMID: 35755027; PMCID: PMC9226906. 10: Frontiers Editorial Office. Expression of Concern: Proxalutamide Reduces the Rate of Hospitalization for COVID-19 Male Outpatients: A Randomized Double- Blinded Placebo-Controlled Trial. Front Med (Lausanne). 2022 Jan 17;8:831449. doi: 10.3389/fmed.2021.831449. PMID: 35111791; PMCID: PMC8802327. 11: Cadegiani FA, Zimerman RA, Fonseca DN, Correia MN, Muller MP, Bet DL, Slaviero MR, Zardo I, Benites PR, Barros RN, Paulain RW, Onety DC, Israel KCP, Gustavo Wambier C, Goren A. Final Results of a Randomized, Placebo-Controlled, Two-Arm, Parallel Clinical Trial of Proxalutamide for Hospitalized COVID-19 Patients: A Multiregional, Joint Analysis of the Proxa-Rescue AndroCoV Trial. Cureus. 2021 Dec 25;13(12):e20691. doi: 10.7759/cureus.20691. PMID: 34976549; PMCID: PMC8712234. 12: Gu Y, Xue M, Wang Q, Hong X, Wang X, Zhou F, Sun J, Wang G, Peng Y. Novel Strategy of Proxalutamide for the Treatment of Prostate Cancer through Coordinated Blockade of Lipogenesis and Androgen Receptor Axis. Int J Mol Sci. 2021 Dec 8;22(24):13222. doi: 10.3390/ijms222413222. PMID: 34948018; PMCID: PMC8704202. 13: Zhang C, Jin H, Wen YF, Yin G. Efficacy of COVID-19 Treatments: A Bayesian Network Meta-Analysis of Randomized Controlled Trials. Front Public Health. 2021 Sep 28;9:729559. doi: 10.3389/fpubh.2021.729559. PMID: 34650951; PMCID: PMC8506153. 14: Cheng Q, Chen J, Jia Q, Fang Z, Zhao G. Efficacy and safety of current medications for treating severe and non-severe COVID-19 patients: an updated network meta-analysis of randomized placebo-controlled trials. Aging (Albany NY). 2021 Sep 16;13(18):21866-21902. doi: 10.18632/aging.203522. Epub 2021 Sep 16. PMID: 34531332; PMCID: PMC8507270. 15: Li H, Song G, Zhou Q, Ran R, Jiang H, Zhang R, Liu Y, Zhang J, Meng L, Ma L, Sun Y, Wang M, Zhou Q, Yan H, Zhou Q, Dong X, Tong Y. Activity of preclinical and phase I clinical trial of a novel androgen receptor antagonist GT0918 in metastatic breast cancer. Breast Cancer Res Treat. 2021 Oct;189(3):725-736. doi: 10.1007/s10549-021-06345-x. Epub 2021 Aug 14. PMID: 34392453; PMCID: PMC8505310. 16: Şimşek-Yavuz S, Komsuoğlu Çelikyurt FI. An update of anti-viral treatment of COVID-19. Turk J Med Sci. 2021 Dec 17;51(SI-1):3372-3390. doi: 10.3906/sag-2106-250. PMID: 34391321; PMCID: PMC8771049. 17: McCoy J, Goren A, Cadegiani FA, Vaño-Galván S, Kovacevic M, Situm M, Shapiro J, Sinclair R, Tosti A, Stanimirovic A, Fonseca D, Dorner E, Onety DC, Zimerman RA, Wambier CG. Proxalutamide Reduces the Rate of Hospitalization for COVID-19 Male Outpatients: A Randomized Double-Blinded Placebo-Controlled Trial. Front Med (Lausanne). 2021 Jul 19;8:668698. doi: 10.3389/fmed.2021.668698. Retraction in: Front Med (Lausanne). 2022 Jun 10;9:964099. doi: 10.3389/fmed.2022.964099. PMID: 34350193; PMCID: PMC8326462. 18: Cadegiani FA, Goren A, Wambier CG, McCoy J. Early COVID-19 therapy with azithromycin plus nitazoxanide, ivermectin or hydroxychloroquine in outpatient settings significantly improved COVID-19 outcomes compared to known outcomes in untreated patients. New Microbes New Infect. 2021 Sep;43:100915. doi: 10.1016/j.nmni.2021.100915. Epub 2021 Jul 7. PMID: 34249367; PMCID: PMC8262389. 19: Novel Agents Show Promise Against Acquired Endocrine Resistance in ER+ Advanced Breast Cancer. Oncologist. 2021 Jul;26 Suppl 3(Suppl 3):S15-S16. doi: 10.1002/onco.13874. Epub 2021 Jun 26. PMID: 34173302; PMCID: PMC8262303. 20: Cadegiani F, Lin EM, Goren A, Wambier CG. Potential risk for developing severe COVID-19 disease among anabolic steroid users. BMJ Case Rep. 2021 Feb 26;14(2):e241572. doi: 10.1136/bcr-2021-241572. Retraction in: BMJ Case Rep. 2023 Nov 9;16(11):e241572ret. doi: 10.1136/bcr-2021-241572ret. Erratum in: BMJ Case Rep. 2023 Nov 2;16(11):e241572corr1. doi: 10.1136/bcr-2021-241572corr1. PMID: 33637513; PMCID: PMC7919571.