52806-53-8 Usage
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
Different sources of media describe the Uses of 52806-53-8 differently. You can refer to the following data:
1. Shown to be an antianhydrogen. The active metabolite of the widely used non-steroidal antagonist flutamide
2. HYDROXYFLUTAMIDE is used non-steroidal antagonist Flutamide. Shown to be an antianhydrogen.
3. 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.
Check Digit Verification of cas no
The CAS Registry Mumber 52806-53-8 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 5,2,8,0 and 6 respectively; the second part has 2 digits, 5 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 52806-53:
(7*5)+(6*2)+(5*8)+(4*0)+(3*6)+(2*5)+(1*3)=118
118 % 10 = 8
So 52806-53-8 is a valid CAS Registry Number.
InChI:InChI=1/C11H11F3N2O4/c1-10(2,18)9(17)15-6-3-4-8(16(19)20)7(5-6)11(12,13)14/h3-5,18H,1-2H3,(H,15,17)
52806-53-8Relevant articles and documents
Method of treatment for prostatic cancer
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, (2008/06/13)
Disclosed is a new treatment for men with prostatic cancer involving combination therapy of a 5α-reductase inhibitor, i.e., a 17β-substituted 4-azasteroid, a 17β-substituted non-azasteroid, 17β-acyl-3-carboxyandrost-3,5-diene, benzoylaminophenoxybutanoic acid derivative, fused benz(thio)amide or cinnamoylamide derivative, aromatic 1,2-diethers or thioethers, aromatic ortho acylaminophenoxy alkanoic acids, ortho thioalkylacylamino-phenoxy alkanoic acids, pharmaceutically acceptable salts and esters thereof, and particularly finasteride, in combination with an antiandrogen, i.e. flutamide. Pharmaceutical compositions useful for treatment are also disclosed.
Combination with anti-hormonal compounds and binding molecules for the treatment of cancer
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, (2008/06/13)
The invention refers to a combination comprising an anti-hormonal compound and a binding molecule specifically binding a c-erb B-2 protein wherein the binding molecule may induce inhibition of tumor cell proliferation., The combination of the invention may be used as medicament for a therapeutic application for treating cancer, wherein the anti-hormonal compound and the binding molecule are administered simultaneously, separately or sequentially.
