1610537-15-9

1610537-15-9 structure

Name: VT-464
Chemical Name: VT-464
CAS Number: 1610537-15-9
Molecular Formula: C₁₈H₁₇F₄N₃O₃
Molecular Weight: 399.340
Catalog: Signaling Pathways Metabolic Enzyme/Protease Cytochrome P450
Create Date: 2018-10-17 17:41:44
Modify Date: 2024-02-07 17:00:51
Seviteronel (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.

Name	VT-464
Synonyms	seviteronel MFCD28167778 (1S)-1-[6,7-Bis(difluoromethoxy)-2-naphthyl]-2-methyl-1-(1H-1,2,3-triazol-4-yl)-1-propanol 8S5OIN36X4 1H-1,2,3-Triazole-4-methanol, α-[6,7-bis(difluoromethoxy)-2-naphthalenyl]-α-(1-methylethyl)-, (αS)-

Description	Seviteronel (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.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450 Research Areas >> Cancer
Target	IC50: 69 nM(h-CYP17 Lyase)[1].
In Vitro	Seviteronel (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[2].
In Vivo	The 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 [2].
References	[1]. Rafferty SW, et al. Highly-selective 4-(1,2,3-triazole)-based P450c17a 17,20-lyase inhibitors. Bioorg Med Chem Lett. 2014 Jun 1;24(11):2444-7. [2]. Sankar N. Maity, et al. Abstract 4772: Efficacy of VT-464, a novel selective inhibitor of cytochrome P450 17,20-lyase, in castrate-resistant prostate cancer models. Cancer Research: April 15, 2013; Volume 73, Issue 8, Supplement 1

Density	1.4±0.1 g/cm3
Boiling Point	536.3±45.0 °C at 760 mmHg
Molecular Formula	C₁₈H₁₇F₄N₃O₃
Molecular Weight	399.340
Flash Point	278.2±28.7 °C
Exact Mass	399.120605
LogP	3.31
Vapour Pressure	0.0±1.5 mmHg at 25°C
Index of Refraction	1.562

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