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  3. VPC-14449

VPC-14449 

Cat. No.: HY-116501
Handling Instructions

VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD), with IC50 of 0.34 μM for full-length human AR. VPC-14449 reduces the ability of full-length AR as well as AR variants to interact with chromatin. VPC-14449 can be used for the research of prostate cancer.

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

VPC-14449 Chemical Structure

VPC-14449 Chemical Structure

CAS No. : 1621375-32-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 330 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD), with IC50 of 0.34 μM for full-length human AR. VPC-14449 reduces the ability of full-length AR as well as AR variants to interact with chromatin. VPC-14449 can be used for the research of prostate cancer[1][2].

IC50 & Target

IC50: 0.34 μM (AR-DBD)[1]

In Vitro

VPC-14449 (0.01-100 μM; 24 h) inhibits AR-transcriptional activity and cell viability in LNCaP, C4-2, MR49F, and 22Rv1 cells[2].
VPC-14449 (0.01-100 μM; 24 h) dose-dependently inhibits the transiently expressed full-length human AR in PC3 cells (IC50=0.34 μM) without affecting AR protein expression[1].

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

Cell Viability Assay[2]

Cell Line: LNCaP, C4-2, MR49F, and 22Rv1 cells
Concentration: 0.01, 0.1, 10, 100 μM
Incubation Time: 24 hours
Result: Suppressed the growth of every tested cell line.

Western Blot Analysis[2]

Cell Line: LNCaP, C4-2, MR49F, and 22Rv1 cells
Concentration: 0.01, 0.1, 10, 100 μM
Incubation Time: 24 hours
Result: Inhibited endogenous AR transactivation in LNCaP, C4-2 and MR49F cells stimulated with the synthetic androgen R1881.
In Vivo

VPC-14449 (100 mg/kg; i.p. twice daily for 4 weeks) reduces tumor volume and abolishes PSA production with no decrease in body weight over a total duration 4 weeks in LNCaP xenograft model[1].

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

Animal Model: Nude mice (Harlan Sprague-Dawley; 25-31 g; 6-8 weeks) were subcutaneously inoculated with LNCaP cells and castrated[1]
Dosage: 100 mg/kg
Administration: I.p. twice daily for 4 weeks
Result: Suppressed LNCaP tumor volume and blocked serum PSA production.
Molecular Weight

394.09

Formula

C₁₀H₁₀Br₂N₄OS

CAS No.
SMILES

BrC1=CN(C2=CSC(N3CCOCC3)=N2)C(Br)=N1

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 : 125 mg/mL (317.19 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5375 mL 12.6875 mL 25.3749 mL
5 mM 0.5075 mL 2.5375 mL 5.0750 mL
10 mM 0.2537 mL 1.2687 mL 2.5375 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: ≥ 2.08 mg/mL (5.28 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.28 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (5.28 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

VPC-14449VPC14449VPC 14449Androgen ReceptorDNAdomainandrogenAR-DBDprostatecancerInhibitorinhibitorinhibit

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Product Name:
VPC-14449
Cat. No.:
HY-116501
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