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Seviteronel racemate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Seviteronel racemate图片
CAS NO:1375603-36-3
规格:98%
分子量:399.34
包装与价格:
包装价格(元)
200mg电议
500mg电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Seviteronel racemate (VT-464 racemate) 消旋体是 Seviteronel (VT-464) 的外消旋形式。
CAS:1375603-36-3
分子式:C18H17F4N3O3
分子量:399.34
纯度:98%
存储:Store at -20°C

Background:

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. IC50: 69 nM(VT-464, h-CYP17 Lyase)[1].


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 on tumor growth of a mCRPC xenograft, MDA-PCa-133, in vivo, and on androgen signaling in C4-2B prostate cancer cells in vitro [2].


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].


[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