5.32996

Androgen Receptor DBD Inhibitor, VPC-14449

• Sinónimos: Androgen Receptor DBD Inhibitor, VPC-14449, AR-DBD Inhibitor, VPC-14449, VPC14449, VPC 14449
• Fórmula empírica (notación de Hill): C₁₀H₁₀Br₂N₄OS
• Número CAS: 1621375-32-3
• Peso molecular: 394.09
• MDL number: MFCD32206764
• UNSPSC Code: 12352200
• NACRES: NA.77
• PubChem Substance ID: 135150480
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Propiedades

• assay: ≥98% (HPLC)
• Quality Segment: 100
• form: solid
• potency: 947 nM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: off-white
• solubility: DMSO: 50 mg/mL
• storage temp.: 2-8°C
• SMILES string: C1COCCN1C2=NC(=CS2)N3C=C(N=C3Br)Br
• 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
• InChI key: AZLNRGRZOLVWRX-UHFFFAOYSA-N

Descripción

General description

A cell-permeable morpholinyl thiazole compound that selectively binds to the DNA-binding domain of androgen receptor (AR) and blocks its activity (IC₅₀ = 340 nM in PC3 cells). Its inhibitory effect is comparable to enzalutamide (IC₅₀ = 314 nM). Does not affect Y594D and Q592D mutant forms of AR. However, Y594A and Q592A mutant AR activity can be inhibited at much higher concentrations (3 - 6 mM). Shown to down-regulate the expression of AR-responsive genes in LNCaP Cells, however, it does not affect genotoxin-responsive genes expression. Suppresses the growth of androgen-sensitive LNCaP xenografts in mice (~100 mg/kg, i.p., b.i.d.).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

VPC-14449, is a cell-permeable compound that selectively binds to the DNA-binding domain of androgen receptor (AR) and blocks its activity (IC₅₀ = 340 nM in PC3 cells).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Androgen Receptor

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Dalal, K., et al. 2014. J. Biol. Chem.289, 26417.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Información de seguridad

• Clase de almacenamiento: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable