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530152 Cdc42/Rac1 Dual Inhibitor, AZA1 - Calbiochem

530152
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₂H₂₀N₆

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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
      Quality LevelMQ100
      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.