VT-464 Racemate

VT-464 Racemate is the racemate form of Seviteronel and is a potent inhibitor of CYP17 lyase.

Product information

CAS Number: 1375603-36-3

Molecular Weight: 399.34

Formula: C18H17F4N3O3

Synonym:

Seviteronel racemate

Chemical Name: 1-[6,7-bis(difluoromethoxy)naphthalen-2-yl]-2-methyl-1-(2H-1,2,3-triazol-4-yl)propan-1-ol

Smiles: CC(C)C(O)(C1C=NNN=1)C1=CC=C2C=C(OC(F)F)C(=CC2=C1)OC(F)F

InChiKey: ZBRAJOQFSNYJMF-UHFFFAOYSA-N

InChi: InChI=1S/C18H17F4N3O3/c1-9(2)18(26,15-8-23-25-24-15)12-4-3-10-6-13(27-16(19)20)14(28-17(21)22)7-11(10)5-12/h3-9,16-17,26H,1-2H3,(H,23,24,25)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 50 mg/mL (125.21 mM); H2O: < 0.1 mg/mL (insoluble)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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). Selective Seviteronel (VT-464) CYP17 lyase inhibition is as effective as AA CYP17 inhibition in this model.

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

Products are for research use only. Not for human use.