532996 Androgen Receptor DBD Inhibitor, VPC-14449 - Calbiochem

532996
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₀H₁₀Br₂N₄OS

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.32996.0001
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          Glass bottle 10 mg
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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
          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.