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533379 p21-Activated Kinase Inhibitor III, FRAX597 - CAS 1286739-19-2 - Calbiochem

533379
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Empirical FormulaCAS #
C₂₉H₂₈ClN₇OS 1286739-19-2

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      Description
      OverviewA cell-permeable, orally bioavailable, pyridopyrimidinone compound that acts as a potent, reversible, and ATP-competitive isoforms selective inhibitor of p21 activated kinase (PAK; IC50 = 7.7, 12.8, and 19.3 nM for PAK1, 2, and 3, respectively). Binds to the back cavity of the ATP binding site of PAK1, and exhibits much reduced activity towards V342F and V342Y mutant forms of PAK1 (IC50 = 3 and 2 µM, respectively). Does not affect the activity of PAK4, 6, and 7 (IC50 > 10 µM). At higher concentrations (100 nM), is shown to cause over 80% inhibition of YES1, RET, CSF1R, and TEK. Reported to block the proliferation of schwannoma cell proliferation by blocking cell cycle at G1 phase. Also blocks the neurofibromatosis 2 (NF2)-associated tumor growth in mice (100 mg/kg, oral for 14 days).

      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 Number533379
      Brand Family Calbiochem®
      Synonyms6-(2-Chloro-4-(thiazol-5-yl)phenyl)-8-ethyl-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrido[2,3-d]pyrimidin-7(8H)-one, PAK Inhibitor III, FRAX-597
      References
      ReferencesLicciulli, S., et al. 2013. J. Biol. Chem. 288, 29105.
      Chow, H.Y., et al. 2012. Cancer Res. 72, 5966.
      Product Information
      CAS number1286739-19-2
      FormOff-white solid
      Hill FormulaC₂₉H₂₈ClN₇OS
      Chemical formulaC₂₉H₂₈ClN₇OS
      Hygroscopic Hygroscopic
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Targetp21 activated kinase
      Primary Target IC<sub>50</sub>7.7, 12.8, and 19.3 nM for PAK1, 2, and 3, respectively
      Purity≥97% 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
      Hygroscopic Hygroscopic
      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

      p21-Activated Kinase Inhibitor III, FRAX597 - CAS 1286739-19-2 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Licciulli, S., et al. 2013. J. Biol. Chem. 288, 29105.
      Chow, H.Y., et al. 2012. Cancer Res. 72, 5966.
      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
      Synonyms6-(2-Chloro-4-(thiazol-5-yl)phenyl)-8-ethyl-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrido[2,3-d]pyrimidin-7(8H)-one, PAK Inhibitor III, FRAX-597
      DescriptionA cell-permeable, orally bioavailable, pyridopyrimidinone compound that acts as a potent, reversible, and ATP-competitive isoforms selective inhibitor of p21 activated kinase (PAK; IC50 = 7.7, 12.8, and 19.3 nM for PAK1, 2, and 3, respectively). Binds to the back cavity of the ATP binding site of PAK1, and exhibits much reduced activity towards V342F and V342Y mutant forms of PAK1 (IC50 = 3 and 2 µM, respectively). Does not affect the activity of PAK4, 6, and 7 (IC50 > 10 µM). At higher concentrations (100 nM), is shown to cause over 80% inhibition of YES1, RET, CSF1R, and TEK. Reported to block the proliferation of schwannoma cell proliferation by blocking cell cycle at G1 phase. Also blocks the neurofibromatosis 2 (NF2)-associated tumor growth in mice (100 mg/kg, oral for 14 days).
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1286739-19-2
      Chemical formulaC₂₉H₂₈ClN₇OS
      Purity≥97% by HPLC
      SolubilityDMSO (10 mg/ml)
      Storage +2°C to +8°C
      Hygroscopic
      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
      ReferencesLicciulli, S., et al. 2013. J. Biol. Chem. 288, 29105.
      Chow, H.Y., et al. 2012. Cancer Res. 72, 5966.