產品屬性：
產品名稱 | Seviteronel racemate |
規格 | 10mM*1mL in DMSO、2mg、5mg、10mg、50mg、100mg、200mg、500mg |
貨號 | EY-01Y17134 |
Cas No.: 1375603-36-3
別名: N/A
化學名: N/A
分子式: C18H17F4N3O3
分子量: 399.34
溶解度: DMSO: 50 mg/mL (125.21 mM); H2O: < 0.1 mg/mL (insoluble)
儲存條件: Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產品描述：
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
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