SCH-451659
SCH-451659 (STX1383) is an orally active, selective 17β-HSD3 inhibitor with an IC50 of 2.4 nM against h17β-HSD3. SCH-451659 selectively blocks the conversion of androstenedione to testosterone. SCH-451659 reduces testosterone levels in mice. SCH-451659 exhibits anticancer activity against androstenedione-dependent prostate tumors.
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- CAS No.: 502628-66-2
- Formule: C30H39Cl2N3O2
- Masse moléculaire:544.56
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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h17β-HSD3 2.4 nM (IC50) |
SCH-451659 potently inhibits h17β-HSD3 in 293-EBNA (HSD3) cells with an IC50 of 2.4 nM, while it exhibits only extremely weak activity against 17β-HSD1 in T47D cells and 17β-HSD2 in MDA-MB-231 cells[1].
SCH-451659 (96 h) inhibits the proliferation of LNCaPwt and PC-3 prostate cancer cells, with IC50 values of 5.9 μM and 5.8 μM against the two cell lines within 96 hours[1].
SCH-451659 (500 nM; for 15 consecutive days) inhibits the proliferation of LNCaP (HSD3) prostate cancer cells stimulated by 10 nM adione[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP(HSD3) prostate cancer cells
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Concentration:500 nM (alongside 10 nM adione stimulation)
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Incubation Time:over15 days
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Result:Inhibited 10 nM adione-stimulated LNCaP(HSD3) cell proliferation by 99.8%.
Did not stimulate or inhibit cell proliferation in the absence of adione.
SCH-451659 (20 mg/kg, subcutaneous injection, administered on days 1-5 and 8-12 for a total of 12 days) significantly reduces plasma testosterone levels in normal male MF-1 nude mice, decreasing them to 17.4% of the control group concentration[1].
SCH-451659 (15 mg/kg; p.o.; twice daily; for 4 weeks) reduces serum testosterone levels by 50%, testicular testosterone levels by 85%, and prostate weight by 20% in cynomolgus monkeys[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MF-1 nude mice (male, castrated, inoculated s.c. with 1×107 LNCaP(HSD3) cells, TP-stimulated then switched to adione stimulation)[1]
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Dosage:20 mg/kg
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Administration:s.c.; daily; 5 weeks
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Result:Inhibited adione-dependent tumour growth significantly, with final tumour volume reaching 326.2 mm3 at day 35 (vs 592.5 mm3 in adione-only controls, P<0.05).
Reduced plasma testosterone concentration to 4.8 ng/mL.
Left mouse body weights unaffected.
Kept 17β-HSD3 and androgen receptor mRNA expression in tumours unchanged relative to in vitro LNCaP(HSD3) cells.
Chemical Information
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CAS No. 502628-66-2
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Masse moléculaire 544.56
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Formule C30H39Cl2N3O2
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SMILES
CC(C)(C)[C@@H]1N(CCN(C1)C(C2=CC=C(C=C2)Cl)C3=CC=C(C=C3)Cl)C(CC4CCN(CC4)C(C)=O)=O
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Synonyms
STX1383
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Day JM, et al. STX2171, a 17β-hydroxysteroid dehydrogenase type 3 inhibitor, is efficacious in vivo in a novel hormone-dependent prostate cancer model. Endocr Relat Cancer. 2013;20(1):53-64. Published 2013 Feb 18. [Content Brief]
[2]. Vicker N, et al. The design of novel 17beta-hydroxysteroid dehydrogenase type 3 inhibitors. Mol Cell Endocrinol. 2009;301(1-2):259-265. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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