VT-464 manufacturers
- Seviteronel
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- $113.00 / 1mg
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2025-11-10
- CAS:1610537-15-9
- Min. Order:
- Purity: 99.98%
- Supply Ability: 10g
- Seviteronel
-
- $113.00 / 1mg
-
2025-11-10
- CAS:1610537-15-9
- Min. Order:
- Purity: 99.98%
- Supply Ability: 10g
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| Product Name: | VT-464 | | Synonyms: | VT-464;Seviteronel;1H-1,2,3-Triazole-5-methanol, α-[6,7-bis(difluoromethoxy)-2-naphthalenyl]-α-(1-methylethyl)-, (αS)-;CS-1247;SEVITERONEL (VT-464);(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 | | EINECS: | | | Product Categories: | | | 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 |
| | VT-464 Preparation Products And Raw materials |
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