Seviteronel - 10mM in DMSO , Androgen Receptor antagonist, CAS No.1610537-15-9, Androgen Receptor antagonist

CAS: 1610537-15-9 Cat. No.: S656033 Fórmula: C₁₈H₁₇F₄N₃O₃ Peso molecular: 399.34 PubChem CID: 78357816

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

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<0.05). These results indicate that selective Seviteronel (VT-464) CYP17 lyase inhibition is as effective as AA CYP17 inhibition in this model . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:IC50: 69 nM(h-CYP17 Lyase)

Specifications

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

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.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Tipo de acción

INHIBITOR

Mecanismo de acción

Androgen Receptor antagonist

Propiedades del producto

• ALogP: 4.7

Nombres e identificadores

• Isómeros SMILES: CC(C)[C@](C1=CC2=CC(=C(C=C2C=C1)OC(F)F)OC(F)F)(C3=NNN=C3)O
• PubChem CID: 78357816
• Peso molecular: 399.34