VT-464 (raceMate)
VT-464 (raceMate) Basic information
- Product Name:
- VT-464 (raceMate)
- Synonyms:
-
- VT-464 (raceMate)
- CS-1246
- Seviteronel racemate
- 1H-1,2,3-Triazole-5-methanol, α-[6,7-bis(difluoromethoxy)-2-naphthalenyl]-α-(1-methylethyl)-
- CAS:
- 1375603-36-3
- MF:
- C18H17F4N3O3
- MW:
- 399.35
- Mol File:
- 1375603-36-3.mol
VT-464 (raceMate) 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; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)
- form
- Powder
- pka
- 8.69±0.70(Predicted)
- color
- Light yellow to yellow
VT-464 (raceMate) Usage And Synthesis
Uses
Seviteronel racemate (VT-464 racemate) is the racemate form of Seviteronel (VT-464), which is a potent CYP17 lyase inhibitor(h-Lyase IC50=nM)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, 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. 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
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