VT-464
VT-464 Basic information
- Product Name:
- VT-464
- Synonyms:
-
- SEVITERONEL (VT-464)
- CS-1247
- VT-464
- Seviteronel
- 1H-1,2,3-Triazole-5-methanol, α-[6,7-bis(difluoromethoxy)-2-naphthalenyl]-α-(1-methylethyl)-, (αS)-
- (s)-1-(6,7-bis(difluoromethoxy)naphthalen-2-yl)-2-methyl-1-(1h-1,2,3-triazol-4-yl)propan-1-ol
- CAS:
- 1610537-15-9
- MF:
- C18H17F4N3O3
- MW:
- 399.35
- Mol File:
- 1610537-15-9.mol
VT-464 Chemical Properties
- Boiling point:
- 536.3±45.0 °C(Predicted)
- Density
- 1.393±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: ≥ 50 mg/mL (125.21 mM)
- pka
- 8.69±0.70(Predicted)
- form
- Powder
- color
- White to light yellow
VT-464 Usage And Synthesis
Uses
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.
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].
IC 50
CYP17
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. DOI:10.1016/j.bmcl.2014.04.024
[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. DOI:10.3389/fendo.2020.00035
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