| 中文名称 |
Seviteronel
|
| 中文别名 |
VT-464
|
| 英文名称 |
Seviteronel
|
| 英文别名 |
VT-464;Seviteronel;VT464;8S5OIN36X4;(S)-1-(6,7-bis(difluoromethoxy)naphthalen-2-yl)-2-methyl-1-(1H-1,2,3-triazol-5-yl)propan-1-ol;1H-1,2,3-Triazole-5-methanol, alpha-(6,7-bis(difluoromethoxy)-2-naphthalenyl)-alpha-(1-methylethyl)-, (alphaS)-;1H-1,2,3-Triazole-5-methanol, alpha-[6,7-bis(difluoromethoxy)-2-naphthalenyl]-alpha-(1-methylethyl)-, (alphaS)-;Seviteronel;VT464;VT 464;DB12275;SB17087;Q21098941
|
| Cas No. |
1610537-15-9
|
| 分子式 |
C18H17F4N3O3
|
| 分子量 |
399.34
|
| 包装储存 |
Powder -20°C 3 years;4°C 2 years
|
| 详情描述 |
Seviteronel (VT-464) 是 CYP17 裂解酶抑制剂,对h-Lyase的 IC50 为 69 nM。
|
| 产品详情 |
Seviteronel (VT-464) 是 CYP17 裂解酶抑制剂,对h-Lyase的 IC50 为 69 nM。
|
| 生物活性 |
Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC 50 =69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.
|
| 性状 |
Solid
|
| IC50 & Target[1][2] |
IC50: 69 nM(h-CYP17 Lyase).
|
| 体外研究(In Vitro) |
Seviteronel (VT-464), a non-steroidal small molecule inhibits androgen production without mineralocorticoid excess or cortisol depletion by selective inhibition of CYP17 17,20-lyase. We determined the impact of Seviteronel (VT-464) on tumor growth of a mCRPC xenograft, MDA-PCa-133, in vivo, and on androgen signaling in C4-2B prostate cancer cells in vitro. has not independently confirmed the accuracy of these methods. They are for reference only.
|
| 体内研究(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]. has not independently confirmed the accuracy of these methods. They are for reference only.
|
| 运输条件 |
Room temperature in continental US; may vary elsewhere.
|
| 储存方式 |
Powder -20°C 3 years;4°C 2 years
|
| ClinicalTrial |
|
| 参考文献 |
[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.[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
|
| 溶解度数据 |
In Vitro: DMSO : ≥ 50 mg/mL (125.21 mM)配制储备液
|
[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.[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
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。