530152 Cdc42/Rac1 Dual Inhibitor, AZA1 - Calbiochem

530152
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₂H₂₀N₆

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.30152.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable indolylpyrimidinediamine compound that selectively suppresses upregulation of GTP-bound Rac1 and Cdc42, but not RhoA, in prostate cancer cells upon EGF-stimulation (Effec. Conc. = 20 µM in serum-starved 22Rv1, DU 154, PC-3 cultures), resulting in time- and dose-dependent (2 to 10 µM and up to 72 h) growth inhibition in serum-deprived cultures with or without EGF stimulation. Dual Cdc42/Rac1 inhibition by AZA1 also effectively inhibits prostate cancer cells migration by decreasing cellular F-/G-actin ratio and disabling both filopodia and lamepodia formation. Daily intraperitoneal injection (100 µg/100 µL 30% DMSO/mouse) is shown to suppress 22Rv1 tumor expansion in mice in vivo.
          Catalogue Number530152
          Brand Family Calbiochem®
          SynonymsN²,N⁴-bis(2-Methyl-1H-indol-5-yl)pyrimidine-2,4-diamine, Cdc42 Inhibitor IV, Rac1 Inhibitor V
          References
          ReferencesZins, K., et al. 2013. PLoS One 8, e74924.
          Product Information
          FormLight brown powder
          Hill FormulaC₂₂H₂₀N₆
          Chemical formulaC₂₂H₂₀N₆
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥95% 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 Ambient Temperature Only
          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 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          Cdc42/Rac1 Dual Inhibitor, AZA1 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Zins, K., et al. 2013. PLoS One 8, e74924.
          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.

          Revision28-March-2014 JSW
          SynonymsN²,N⁴-bis(2-Methyl-1H-indol-5-yl)pyrimidine-2,4-diamine, Cdc42 Inhibitor IV, Rac1 Inhibitor V
          DescriptionA cell-permeable indolylpyrimidinediamine compound that selectively suppresses cellular levels of GTP-bound Rac1 and Cdc42, but not RhoA, in serum-starved prostate cancer cultures upon EGF-stimulation (% of non-stimulated control Rac1-GTP level with/without 20 µM AZA1 = 56/375 in 22Rv1, 30/235 in DU 154, and 12/118 in PC-3 cells; % of non-EGF-stimulated control Cdc42-GTP level with/without 20 µM AZA1 = 15/170 in 22Rv1, 30/105 in DU 154, and 12/100 in PC-3 cells), resulting in effective suppression of PAK1, Akt, and BAD phosphorylations, as well as time- and dose-dependent (2 to 10 µM and up to 72 hr) growth inhibition of the cells in serum-deprived cultures with or without EGF stimulation. Dual Cdc42/Rac1 inhibition by AZA1 also effectively inhibits prostate cancer cells migration by decreasing cellular F-/G-actin ratio and disabling both filopodia and lamepodia formation. Daily intraperitoneal injection (100 µg/100 µL 30% DMSO/mouse) is shown to be efficacious in suppressing 22Rv1 tumor expansion in mice in vivo.
          FormLight brown powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₂H₂₀N₆
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (100 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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesZins, K., et al. 2013. PLoS One 8, e74924.