1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. Seviteronel racemate

Seviteronel racemate (Synonyms: VT-464 (racemate))

Cat. No.: HY-15996B Purity: 98.11%
Handling Instructions

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.

For research use only. We do not sell to patients.

Seviteronel racemate Chemical Structure

Seviteronel racemate Chemical Structure

CAS No. : 1375603-36-3

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 462 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 462 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 Get quote
100 mg USD 2520 Get quote
200 mg   Get quote  
500 mg   Get quote  

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Description

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 & Target

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

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 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].

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, 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

399.34

Formula

C18H17F4N3O3

CAS No.
SMILES

FC(F)OC1=C(OC(F)F)C=C(C=CC(C(C2=CNN=N2)(C(C)C)O)=C3)C3=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (125.21 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent 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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3 mg/mL (7.51 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 3 mg/mL (7.51 mM); Clear solution

*All of the co-solvents are available by MCE.
References
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Product Name:
Seviteronel racemate
Cat. No.:
HY-15996B
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