research use only
Cat.No.S1202
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In vitro |
DMSO
: 106 mg/mL
(200.55 mM)
Ethanol : 25 mg/mL Water : Insoluble |
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In vivo |
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| Molecular Weight | 528.53 | Formula | C27H30F6N2O2 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 164656-23-9 | Download SDF | Storage of Stock Solutions |
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| Synonyms | GI198745, GG-745 | Smiles | CC12CCC3C(C1CCC2C(=O)NC4=C(C=CC(=C4)C(F)(F)F)C(F)(F)F)CCC5C3(C=CC(=O)N5)C | ||
| Targets/IC50/Ki |
5-α reductase
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|---|---|
| In vitro |
Dutasteride inhibits type-1 5AR and type-2 5AR with IC50 of 6 nM and 7 nM, respectively. This compound is 60-fold more potent than Finasteride in its initial Ki versus type 1 5AR and ~5-fold more rapid in inactivating the enzyme. This inhibitor inhibits (3)H-T conversion to (3)H-DHT and, as anticipated, inhibits T-induced secretion of PSA and proliferation in LNCaP cells. It also inhibits DHT-induced PSA secretion and cell proliferation with IC50 of 1 μM in LNCaP cells. This compound competes for binding the LNCaP cell AR with an IC50 of 1.5 μM. This chemical (10–50 μM) results in enhanced cell death, possibly by apoptosis, in steroid-free medium. It reduces cell viability and cell proliferation in androgen-responsive (LNCaP) and androgen-unresponsive (DU145) human prostate cancer(PCa) cell lines. This agent 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. This compound inhibits FASN mRNA, protein expression and enzymatic activity in prostate cancer cells. |
| In vivo |
Dutasteride (100 mg/kg/day) has prostates about half as large as those in intact male rats treated with vehicle alone. This compound is orally bioavailable and because of its mechanism of action it easily overcomes the potential liability of being >99% plasma protein bound. |
References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03669692 | Withdrawn | Prostatic Hyperplasia Benign|Metabolic Syndrome |
Complexo Hospitalario Universitario de A Coruña |
July 10 2018 | Not Applicable |
| NCT02839122 | Completed | Benign Prostate Hyperplasia |
Yuyu Pharma Inc. |
May 2016 | Phase 1 |
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