532996 Androgen Receptor DBD Inhibitor, VPC-14449 - Calbiochem

532996
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₀H₁₀Br₂N₄OS

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      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
      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

      Documentation

      Androgen Receptor DBD Inhibitor, VPC-14449 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      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
      Chemical formulaC₁₀H₁₀Br₂N₄OS
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesDalal, K., et al. 2014. J. Biol. Chem. 289, 26417.