| Company Name: |
SPIRO PHARMA |
| Tel: |
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| Email: |
eric_feng1954@126.com |
VT-464 (raceMate) manufacturers
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| | 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 | | EINECS: | | | Product Categories: | | | 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 |
| | VT-464 (raceMate) Preparation Products And Raw materials |
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