5.32996
Androgen Receptor DBD Inhibitor, VPC-14449
Synonym(s):
Androgen Receptor DBD Inhibitor, VPC-14449, AR-DBD Inhibitor, VPC-14449, VPC14449, VPC 14449
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About This Item
Empirical Formula (Hill Notation):
C10H10Br2N4OS
CAS Number:
Molecular Weight:
394.09
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
Recommended Products
assay
≥98% (HPLC)
Quality Level
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
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.
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.
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.
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
Androgen Receptor
Warning
Toxicity: Standard Handling (A)
Reconstitution
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
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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