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.
Product information
CAS Number: 1621375-32-3
Molecular Weight: 394.09
Formula: C10H10Br2N4OS
Chemical Name: 4-[4-(2,4-dibromo-1H-imidazol-1-yl)-1,3-thiazol-2-yl]morpholine
Smiles: BrC1=NC(Br)=CN1C1=CSC(=N1)N1CCOCC1
InChiKey: AZLNRGRZOLVWRX-UHFFFAOYSA-N
InChi: InChI=1S/C10H10Br2N4OS/c11-7-5-16(9(12)13-7)8-6-18-10(14-8)15-1-3-17-4-2-15/h5-6H,1-4H2
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 125 mg/mL (317.19 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. 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.
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.
Products are for research use only. Not for human use.
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