1. Metabolic Enzyme/Protease
  2. Cytochrome P450

VT-464 (Synonyms: Seviteronel)

Cat. No.: HY-15996 Purity: 99.11%
Handling Instructions

VT-464 is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.

For research use only. We do not sell to patients.
VT-464 Chemical Structure

VT-464 Chemical Structure

CAS No. : 1610537-15-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 462 In-stock
5 mg USD 420 In-stock
10 mg USD 600 In-stock
50 mg USD 1800 In-stock
100 mg USD 2520 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other Forms of VT-464:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

VT-464 is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition. IC50 value: 69 nM(h-CYP17 Lyase) [1] Target: CYP17 Lyase inhibitor in vitro: 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 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 [2]. 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 VT464 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 VT-464 and AA reduced tumor volume (>two fold compared to vehicle; p<0.05). These results indicate that selective VT-464 CYP17 lyase inhibition is as effective as AA CYP17 inhibition in this model [2].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.5041 mL 12.5207 mL 25.0413 mL
5 mM 0.5008 mL 2.5041 mL 5.0083 mL
10 mM 0.2504 mL 1.2521 mL 2.5041 mL
Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

399.34

Formula

C₁₈H₁₇F₄N₃O₃

CAS No.

1610537-15-9

SMILES

FC(F)OC1=C(OC(F)F)C=C(C=CC([[email protected]](C2=CNN=N2)(C(C)C)O)=C3)C3=C1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
VT-464
Cat. No.:
HY-15996
Quantity: