| Size | Price | Stock | Qty |
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| 25mg |
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| 100mg |
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Proxalutamide (GT0918; GT-0918) is a novel, oral and potent androgen receptor/AR antagonist or nonsteroidal antiandrogen (NSAA). It is being investigated in phase 1/2/3 clinical trials for treating prostate cancer, breast cancer and COVID-19 pandemic. It was approved in Paraguay for the treatment of COVID-19 in July 2021, but has not been approved at this time in other countries.
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| Additional Infomation |
Proxalutamide is under investigation in clinical trial NCT03899467 (The Safety and Tolerability of Proxalutamide (GT0918) in Subjects With Metastatic Castrate Resistant Prostate Cancer).
Proxalutamide is an orally bioavailable androgen receptor (AR) antagonist with potential antineoplastic activity. Upon oral administration, proxalutamide binds to AR in target tissues, inhibits androgen-induced receptor activation, and facilitates the formation of inactive complexes that cannot translocate to the nucleus. This prevents binding to and transcription of AR-responsive genes that regulate prostate cancer cell proliferation. In addition, proxalutamide induces AR downregulation, thereby further preventing AR-mediated signaling. This ultimately leads to an inhibition of growth in AR-expressing prostate cancer cells. AR is overexpressed in prostate cancer and plays a key role in prostate cancer cell proliferation. Mechanism of Action Proxalutamide is an antagonist at the androgen receptor which leads to inhibition of androgen-induced receptor activation and results in formation of inactive complexes that are not able to translocate to the nucleus. It also induces androgen receptor downregulation, furthering adrogen-induced receptor activation. This drug is being investigated for its potential antineoplastic activity and is being investigated specifically against prostate cancer and COVID-19. |
| Molecular Formula |
C24H19F4N5O2S
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| Molecular Weight |
517.4986
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| Exact Mass |
517.119
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| Elemental Analysis |
C, 55.70; H, 3.70; F, 14.68; N, 13.53; O, 6.18; S, 6.20
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| CAS # |
1398046-21-3
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| PubChem CID |
60194102
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| Appearance |
Solid powder
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| LogP |
4.3
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
36
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| Complexity |
894
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KCBJGVDOSBKVKP-UHFFFAOYSA-N
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| 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
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| 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
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| Synonyms |
Proxalutamide GT 0918 GT0918GT-0918
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9324 mL | 9.6618 mL | 19.3237 mL | |
| 5 mM | 0.3865 mL | 1.9324 mL | 3.8647 mL | |
| 10 mM | 0.1932 mL | 0.9662 mL | 1.9324 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04728802 | COMPLETEDWITH RESULTS | Drug: Proxalutamide Drug: Placebo |
Covid19 SARS (Severe Acute Respiratory Syndrome) |
Applied Biology, Inc. | 2021-02-01 | Phase 3 |
| NCT04853134 | WITHDRAWN | Drug: Proxalutamide Other: Standard of Care |
Covid19 SARS-CoV Infection |
Applied Biology, Inc. | 2020-11-01 | Phase 3 |
| NCT04103853 | COMPLETED | Drug: Proxalutamide | Metastatic Breast Cancer | Suzhou Kintor Pharmaceutical Inc, | 2017-09-06 | Phase 1 |
| NCT04853927 | WITHDRAWN | Drug: Proxalutamide Drug: Placebo |
Covid19 SARS (Severe Acute Respiratory Syndrome) |
Applied Biology, Inc. | 2021-02-08 | Phase 3 |
| NCT05126628 | COMPLETED | Drug: Proxalutamide Drug: Placebo |
COVID-19 | Corpometria Institute | 2021-03-06 | Phase 3 |
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