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. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 IC50& Target:IC50: 69 nM(h-CYP17 Lyase)
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Seviteronel
CAS number：1610537-15-9(DMSO) molecular formula：C18H17F4N3O3
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| Chinese alias | 塞维特罗内尔 | ||
| English alias | - | ||
| CAS number | 1610537-15-9(DMSO) | molecular formula | C18H17F4N3O3 |
| molecular weight | 399.34 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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