Seviteronel

Seviteronel (VT-464) is a potent CYP17 lyase inhibitor (h-Lyase IC50=69 nM) and an AR antagonist. Seviteronel demonstrates both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.

Product Specifications

CAS Number

[1610537-15-9]

Product Name Alternative

VT-464

UNSPSC

12352005

Target

Androgen Receptor; Cytochrome P450

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/VT-464.html

Purity

99.83

Solubility

DMSO : ≥ 50 mg/mL

Smiles

FC(F)OC1=C(OC(F)F)C=C(C=CC([C@](C2=CNN=N2)(C(C)C)O)=C3)C3=C1

Molecular Formula

C18H17F4N3O3

Molecular Weight

399.34

References & Citations

[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|[3]Michmerhuizen AR, et al. Seviteronel, a Novel CYP17 Lyase Inhibitor and Androgen Receptor Antagonist, Radiosensitizes AR-Positive Triple Negative Breast Cancer Cells. Front Endocrinol (Lausanne) . 2020 Feb 11;11:35.