| Identification | Back Directory | [Name]
VT-464 | [CAS]
1610537-15-9 | [Synonyms]
VT-464
CS-1247
Seviteronel
SEVITERONEL (VT-464)
1H-1,2,3-Triazole-5-methanol, α-[6,7-bis(difluoromethoxy)-2-naphthalenyl]-α-(1-methylethyl)-, (αS)- | [Molecular Formula]
C18H17F4N3O3 | [MDL Number]
MFCD28167778 | [MOL File]
1610537-15-9.mol | [Molecular Weight]
399.35 |
| Chemical Properties | Back Directory | [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) | [form ]
Powder | [pka]
8.69±0.70(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [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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SPIRO PHARMA
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www.spiropharma.com.cn |
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Musechem
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+1-800-259-7612 |
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www.musechem.com |
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Cckinase, Inc.
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+1 (732)236-3202 |
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www.cckinase.com |
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