Seviteronel
CAS No. 1610537-15-9
Seviteronel( —— )
Catalog No. M33166 CAS No. 1610537-15-9
Seviteronel (VT-464) is a novel CYP17 cleavage enzyme inhibitor and androgen receptor antagonist used in breast and prostate cancer research.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
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| 50MG | 892 | In Stock |
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| 100MG | 1190 | In Stock |
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Biological Information
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Product NameSeviteronel
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NoteResearch use only, not for human use.
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Brief DescriptionSeviteronel (VT-464) is a novel CYP17 cleavage enzyme inhibitor and androgen receptor antagonist used in breast and prostate cancer research.
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DescriptionSeviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.
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In VitroSeviteronel (VT-464), a non-steroidal small molecule inhibits androgen production without mineralocorticoid excess or cortisol depletion by selective inhibition of CYP17 17,20-lyase. We determined the impact of Seviteronel (VT-464) on tumor growth of a mCRPC xenograft, MDA-PCa-133, in vivo, and on androgen signaling in C4-2B prostate cancer cells in vitro.
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In VivoThe MDA-PCa-133 xenograft is derived from a clinical CRPC bone metastasis. Subcutaneous MDA-PCa-133 tumor expresses PSA, full-length androgen receptor (AR) and AR-V7 isoform. We determined the effect of Seviteronel (VT-464) and AA on MDA-PCa-133 growing in tumor-bearing castrated male mice: randomization into three groups; oral treatment with vehicle only, VT-464, (100 mg/kg bid), or AA (100 mg/kg bid) for 25 days. Both Seviteronel (VT-464)and AA reduced tumor volume (>two fold compared to vehicle; p<0.05). These results indicate that selective Seviteronel (VT-464)CYP17 lyase inhibition is as effective as AA CYP17 inhibition in this model .
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Synonyms——
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PathwayMetabolic Enzyme/Protease
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TargetP450
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RecptorP450 | Androgen Receptor
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Research Area——
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Indication——
Chemical Information
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CAS Number1610537-15-9
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Formula Weight399.34
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Molecular FormulaC18H17F4N3O3
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : ≥ 50 mg/mL (125.21 mM)
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SMILESCC(C)[C@@](O)(c1c[nH]nn1)c1ccc2cc(OC(F)F)c(OC(F)F)cc2c1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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Harman hydrochloride
Harman hydrochloride can directly induce CYP1A1 gene expression in an AhR-dependent manner and may represent a novel mechanism by which harman promotes mutagenicity, co-mutagenicity and carcinogenicity.
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EN3356
EN3356 is an orally available and selective inhibitor of steroidal 17-alpha-hydroxylase/C17,20 cleavage enzyme (CYP17A1 or CYP17), a non-steroidal cleavage enzyme-selective compound with potential anti-androgenic and anti-tumor activity.
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PF-4981517
PF-4981517 (CYP3cide) is a efficient, specific and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC 50 values for CYP3A activity are 0.03 μM,17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively.
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