Proxalutamide (CAT: I008887) is a novel androgen receptor antagonist that exhibits anti-androgenic effects. It selectively binds to androgen receptors, inhibiting the binding of endogenous androgens and the activation of androgen receptor signaling. Proxalutamide has shown promise in the treatment of prostate cancer by suppressing tumor growth and inhibiting androgen receptor-mediated signaling pathways. Additionally, it has potential applications in the management of androgen-dependent conditions, such as androgenic alopecia and hirsutism. Clinical trials are underway to evaluate the efficacy, safety, and optimal dosage of proxalutamide in various androgen-related disorders, providing a potential therapeutic option for patients in need.
| Catalog Number | I008887 |
| CAS Number | 1398046-21-3 |
| Synonyms | Proxalutamide; GT-0918; GT 0918; GT0918;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 |
| Molecular Formula | C24H19F4N5O2S |
| Purity | ≥95% |
| Target | Androgen Receptor Antagonist |
| Solubility | Soluble in DMSO |
| Storage | 0 - 4 °C for short term, or -20 °C for long term |
| IUPAC Name | 4-[4,4-dimethyl-3-[6-[3-(1,3-oxazol-2-yl)propyl]pyridin-3-yl]-5-oxo-2-sulfanylideneimidazolidin-1-yl]-3-fluoro-2-(trifluoromethyl)benzonitrile |
| InChI | 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 |
| InChIKey | KCBJGVDOSBKVKP-UHFFFAOYSA-N |
| SMILES | CC1(C(=O)N(C(=S)N1C2=CN=C(C=C2)CCCC3=NC=CO3)C4=C(C(=C(C=C4)C#N)C(F)(F)F)F)C |
| Reference | </br>1: Yang M, He S, Fan Y, Wang Y, Ge Z, Shan L, Gong W, Huang X, Tong Y, Gao C. Microenvironmental pH-modified solid dispersions to enhance the dissolution and bioavailability of poorly water-soluble weakly basic GT0918, a developing anti-prostate cancer drug: preparation, characterization and evaluation in vivo. Int J Pharm. 2014 Nov 20;475(1-2):97-109. doi: 10.1016/j.ijpharm.2014.08.047. PubMed PMID: 25171976.</br>2: Peng Y, Wu H, Zhang X, Zhang F, Qi H, Zhong Y, Wang Y, Sang H, Wang G, Sun J. A comprehensive assay for nine major cytochrome P450 enzymes activities with 16 probe reactions on human liver microsomes by a single LC/MS/MS run to support reliable in vitro inhibitory drug-drug interaction evaluation. Xenobiotica. 2015;45(11):961-77. doi: 10.3109/00498254.2015.1036954. PubMed PMID: 26007223. |
