VPC-14449

SKU: orb1702675

Description

VPC-14449 is a selective small molecule inhibitor targeting the DNA-binding domain (DBD) of the androgen receptor (AR). It is utilized in prostate cancer research to study AR signaling and has demonstrated activity in disrupting AR-DNA interactions in both cellular and animal models.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1621375-32-3
• MW: 394.09
• Purity: 99.56% (May vary between batches)
• Formula: C₁₀H₁₀Br₂N₄OS
• SMILES: BrC=1N=C(Br)N(C1)C=2N=C(SC2)N3CCOCC3
• Target: Androgen Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (10.15 mM);DMSO:100 mg/mL (253.75 mM)

Bioactivity

• Target IC50:
  AR-DBD:0.34 μM
• In Vivo:
  Methods: Castrated mice were given VPC-14449 (100 mg/kg, ip, for 4 weeks) twice daily and LNCaP xenograft tumor volume and serum PSA were assessed. Results: VPC-14449 reduced tumor volume and abolished PSA production in the LNCaP xenograft model.
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• In Vitro:
  Methods: LNCaP, C4-2, MR49F, and 22Rv1 cells were treated with VPC-14449 (0.01-100 μM, 24 hours) to test its inhibitory effect on AR-V7 transcriptional activity in cells. Results: VPC-14449 inhibited AR transcriptional activity and cell viability in LNCaP, C4-2, MR49F, and 22Rv1 cells.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

VPC 14449, VPC14449, VPC-14449

Compound Identifiers

PubChem CID

135150480