Chemical Property of Hydroxyflutamide
Chemical Property:
- Appearance/Colour:Yellow-Brown Powder
- Melting Point:125-130°C
- Boiling Point:443.801 °C at 760 mmHg
- PKA:12.87±0.70(Predicted)
- Flash Point:222.203 °C
- PSA：95.15000
- Density:1.472g/cm3
- LogP:2.91920
- Storage Temp.:-20°C Freezer
- Solubility.:DMSO: >10mg/mL
- XLogP3:2.2
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:7
- Rotatable Bond Count:2
- Exact Mass:292.06709132
- Heavy Atom Count:20
- Complexity:392
- Purity/Quality:
-
97% *data from raw suppliers
Hydroxyflutamide *data from reagent suppliers
Safty Information:
- Pictogram(s):
Xi
- Hazard Codes:Xi
- Statements:
36/37/38
- Safety Statements:
26-36/37/39
- MSDS Files:
-
SDS file from LookChem
Total 1 MSDS from other Authors
Useful:
- Canonical SMILES:CC(C)(C(=O)NC1=CC(=C(C=C1)[N+](=O)[O-])C(F)(F)F)O
- Recent ClinicalTrials:A Study of 2-hydroxyflutamide (Liproca Depot), Injected Into the Prostate in Patients With Localized Prostate Cancer
- Recent EU Clinical Trials:A Single Blind, Two-Stage Dose Finding Study to Evaluate the Safety, Tolerability and Efficacy of a Single Liproca? Depot Injection into the Prostate in Patients with Localized Prostate Cancer, Assigned to Active Surveillance who are at High Risk for Disease Progression (followed by an Open Label Extension with a Repeat Injection (Optional)).
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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.
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Uses
Shown to be an antianhydrogen. The active metabolite of the widely used non-steroidal antagonist flutamide HYDROXYFLUTAMIDE is used non-steroidal antagonist Flutamide. Shown to be an antianhydrogen. The active metabolite of the widely used non-steroidal antagonist Flutamide (F598850). Shown to be an antianhydrogen.
