Dutasteride

Catalog No.S1202 Batch:S120203

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Technical Data

Formula

C27H30F6N2O2
Molecular Weight 528.53 CAS No. 164656-23-9
Solubility (25°C)* In vitro DMSO 100 mg/mL (189.2 mM)
Ethanol 13 mg/mL (24.59 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Dutasteride (GI198745, GG-745) is a dual 5-α reductase inhibitor that inhibits conversion of testosterone to dihydrotestosterone (DHT).
Targets
5-α reductase [1]
In vitro

Dutasteride inhibits type-1 5AR and type-2 5AR with IC50 of 6 nM and 7 nM, respectively. Dutasteride is 60-fold more potent than Finasteride in its initial Ki versus type 1 5AR and ~5-fold more rapid in inactivating the enzyme. [1]

Dutasteride inhibits (3)H-T conversion to (3)H-DHT and, as anticipated, inhibits T-induced secretion of PSA and proliferation in LNCaP cells. Dutasteride also inhibits DHT-induced PSA secretion and cell proliferation with IC50 of 1 μM in LNCaP cells. Dutasteride competes for binding the LNCaP cell AR with an IC50 of 1.5 μM. Dutasteride (10–50 μM) results in enhanced cell death, possibly by apoptosis, in steroid-free medium. [2]

Dutasteride reduces cell viability and cell proliferation in androgen-responsive (LNCaP) and androgen-unresponsive (DU145) human prostate cancer(PCa) cell lines. Dutasteride results in overexpressed genes included genes encoding for proteins involved in biosynthesis and metabolism of androgen (HSD17B1;HSD17B3;CYP11B2), androgen receptor and androgen receptor co-regulators (AR;CCND1), and signal transduction(ERBB2; V-CAM; SOS1) whereas, underexpressed genes (KLK3; KLK2; DHCR24) are androgen-regulated genes (ARGs) in androgen-responsive (LNCaP) cell. [3]

Dutasteride inhibits FASN mRNA, protein expression and enzymatic activity in prostate cancer cells. [4]
In vivo

Dutasteride (100 mg/kg/day) has prostates about half as large as those in intact male rats treated with vehicle alone. Dutasteride is orally bioavailable and because of its mechanism of action it easily overcomes the potential liability of being >99% plasma protein bound. [1]

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    LNCaP Cells

  • Concentrations

    1 μM

  • Incubation Time

    5 days

  • Method

    Cells were treated with various concentrations of drug for 5 days.
Animal Study:

[5]
  • Animal Models

    Male Sprague-Dawley rats

  • Dosages

    0.5 mg/kg

  • Administration

    i.g. gavage

Selleck's Dutasteride has been cited by 8 publications

An integrated in vitro/in silico approach to assess the anti-androgenic potency of isobavachin [ Food Chem Toxicol, 2023, 176:113764] PubMed: 37019376
Impact of short-term Dutasteride treatment on prostate-specific membrane antigen expression in a mouse xenograft model [ Cancer Rep (Hoboken), 2021, e1418] PubMed: 34008909
Androgen Signaling Regulates SARS-CoV-2 Receptor Levels and Is Associated with Severe COVID-19 Symptoms in Men [ Cell Stem Cell, 2020, 27(6):876-889.e12] PubMed: 33232663
High-throughput liquid chromatography tandem mass spectrometry assay as initial testing procedure for analysis of total urinary fraction [ Drug Test Anal, 2020, 10.1002/dta.2917] PubMed: 32852861
Concentration-dependent effects of dutasteride on prostate-specific membrane antigen (PSMA) expression and uptake of 177 Lu-PSMA-617 in LNCaP cells [ Prostate, 2019, 10.1002/pros.23868] PubMed: 31233227
Inhibition of dihydrotestosterone synthesis in prostate cancer by combined frontdoor and backdoor pathway blockade. [ Oncotarget, 2018, 9(13):11227-11242] PubMed: 29541409
Serum‐free complete medium, an alternative medium to mimic androgen deprivation in human prostate cancer cell line models [Fiandalo MV Prostate, 2018, 78(3):213-221] PubMed: 29194687
Pharmacological upregulation of prostate‐specific membrane antigen (PSMA) expression in prostate cancer cells [Kranzbühler B Prostate, 2018, 78(10):758-765] PubMed: 29633296

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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