1375603-36-3

1375603-36-3 structure

Name: VT-464 (racemate)
Chemical Name: 1-(6,7-bis(difluoromethoxy)naphthalen-2-yl)-2-methyl-1-(1H-1,2,3-triazol-4-yl)propan-1-ol
CAS Number: 1375603-36-3
Molecular Formula: C₁₈H₁₇F₄N₃O₃
Molecular Weight: 399.33900
Catalog: Signaling Pathways Metabolic Enzyme/Protease Cytochrome P450
Create Date: 2017-03-08 14:45:08
Modify Date: 2024-01-09 12:00:40
Seviteronel (VT-464) racemate is the racemate form of Seviteronel (VT-464), which is a potent CYP17 lyase inhibitor(h-Lyase IC50=nM)inhibition.

Name	1-(6,7-bis(difluoromethoxy)naphthalen-2-yl)-2-methyl-1-(1H-1,2,3-triazol-4-yl)propan-1-ol
Synonyms	VT-464 racemate VT-464 (racemate)

Description	Seviteronel (VT-464) racemate is the racemate form of Seviteronel (VT-464), which is a potent CYP17 lyase inhibitor(h-Lyase IC50=nM)inhibition.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450 Research Areas >> Cancer
Target	IC50: 69 nM(VT-464, 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 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, Seviteronel (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

Molecular Formula	C₁₈H₁₇F₄N₃O₃
Molecular Weight	399.33900
Exact Mass	399.12100
PSA	80.26000
LogP	4.05260

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