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532996 Androgen Receptor DBD Inhibitor, VPC-14449 - CAS 1621375-32-3 - Calbiochem

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).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: AR-DBD Inhibitor, VPC-14449, VPC14449, VPC 14449

Primary Target: Androgen Receptor
532996
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1621375-32-3C₁₀H₁₀Br₂N₄OS

Products

Catalogue NumberPackaging Qty/Pack
5.32996.0001 Glass bottle 10 mg
Description
OverviewA 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.
Catalogue Number532996
Brand Family Calbiochem®
SynonymsAR-DBD Inhibitor, VPC-14449, VPC14449, VPC 14449
References
ReferencesDalal, K., et al. 2014. J. Biol. Chem. 289, 26417.
Product Information
CAS number1621375-32-3
FormOff-white solid
Hill FormulaC₁₀H₁₀Br₂N₄OS
Chemical formulaC₁₀H₁₀Br₂N₄OS
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary TargetAndrogen Receptor
Primary Target IC<sub>50</sub>947 nM
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
5.32996.0001 04055977282009

Documentation

Androgen Receptor DBD Inhibitor, VPC-14449 - CAS 1621375-32-3 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Androgen Receptor DBD Inhibitor, VPC-14449 - CAS 1621375-32-3 - Calbiochem Certificates of Analysis

TitleLot Number
532996

References

Reference overview
Dalal, K., et al. 2014. J. Biol. Chem. 289, 26417.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision20-November-2015 JSW
SynonymsAR-DBD Inhibitor, VPC-14449, VPC14449, VPC 14449
DescriptionA 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.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1621375-32-3
Chemical formulaC₁₀H₁₀Br₂N₄OS
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesDalal, K., et al. 2014. J. Biol. Chem. 289, 26417.