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| HYDROXYFLUTAMIDE Basic information |
| HYDROXYFLUTAMIDE Chemical Properties |
| Melting point | 125-130°C | | Boiling point | 443.8±45.0 °C(Predicted) | | density | 1.472 | | storage temp. | room temp | | solubility | DMSO: >10mg/mL | | pka | 12.87±0.70(Predicted) | | form | powder | | color | white to tan |
| Hazard Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 26-36/37/39 | | WGK Germany | 3 | | RTECS | TX1466250 | | HS Code | 2924297099 |
| HYDROXYFLUTAMIDE Usage And Synthesis |
| Description | 2-hydroxy Flutamide is the major metabolite formed during the metabolism of the non-steroidal antiandrogen flutamide by cytochrome P450 (CYP) isoforms CYP1A2 and CYP3A4. Through competitive inhibition of the binding of testosterone to the nuclear androgen receptor (AR; IC50 = ~300-900), 2-hydroxy flutamide blocks the expression of AR target genes and prevents androgen-dependent stabilization of the AR. Compared to flutamide, 2-hydroxy flutamide is a more potent antiandrogen in vivo, demonstrating a higher binding affinity for the AR (0.1% binding affinity relative to dihydrotestosterone) and, thus, is the predominant contributor to the therapeutic effects of flutamide in the treatment of prostate cancer. | | Chemical Properties | HYDROXYFLUTAMIDE is Yellow-Brown Powder
| | Uses | Shown to be an antianhydrogen. The active metabolite of the widely used non-steroidal antagonist flutamide | | Uses | HYDROXYFLUTAMIDE is used non-steroidal antagonist Flutamide. Shown to be an antianhydrogen.
| | Uses | The active metabolite of the widely used non-steroidal antagonist Flutamide (F598850). Shown to be an antianhydrogen. | | Biochem/physiol Actions | Hydroxyflutamide plays a role in preventing the binding of 5α-dihydrotestosterone (DHT) and testosterone to the androgen receptors. | | references | [1] kolvenbag g, furr b j a, blackledge g r p. receptor affinity and potency of non-steroidal antiandrogens: translation of preclinical findings into clinical activity[j]. prostate cancer and prostatic diseases, 1998, 1: 307-314.[2] heinlein c a, chang c. androgen receptor in prostate cancer[j]. endocrine reviews, 2004, 25(2): 276-308.[3] shet m s, mcphaul m, fisher c w, et al. metabolism of the antiandrogenic drug (flutamide) by human cyp1a2[j]. drug metabolism and disposition, 1997, 25(11): 1298-1303.[4] gao w, kim j, dalton j t. pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands[j]. pharmaceutical research, 2006, 23(8): 1641-1658. |
| HYDROXYFLUTAMIDE Preparation Products And Raw materials |
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