500613 p21-Activated Kinase Inhibitor II, PF-3758309 - CAS 898044-15-0 - Calbiochem

500613
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Key Specifications Table

Empirical FormulaCAS #
C₂₅H₃₀N₈OS 898044-15-0

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      Description
      OverviewA cell-permeable pyrrolopyrazole that acts as a potent inhibitor against p21-activated kinases (Ki in nM/[ATP] in µM = 13.7/200, 18.7/40, 18.1/80. 17.1/72, respectively, in PAK1, PAK4, PAK5, PAK6 kinase assays; IC50 = 190 and 99 nM against PAK1 and PAK3, respectively) by directly targeting the kinase ATP-binding site in a reversible manner (Kd = 4.5 nM using rhPAK4300-591 kinase domain). Inhibits PAK4-dependent cellular signaling (IC50 = 24.2 nM against TNFα-stimulated NF-κB activity in HEK293T) and proliferation (IC50 = 0.24 and 27 nM, respectively, against HCT116 and A549 colonies formation) in vitro and the growth of human tumors in nude mice in vivo (10 to 25 mg/kg; b.i.d. p.o).

      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 Number500613
      Brand Family Calbiochem®
      Synonyms(S)-N-(2-(Dimethylamino)-1-phenylethyl)-6,6-dimethyl-3-(2-methylthieno[3,2-d]pyrimidin-4-ylamino)-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, PAK Inhibitor II, PF3758309
      References
      ReferencesMurray, B.W., et al. 2010. Proc. Natl. Acad. Sci. USA. 107, 9446.
      Product Information
      CAS number898044-15-0
      FormYellowish-white powder
      Hill FormulaC₂₅H₃₀N₈OS
      Chemical formulaC₂₅H₃₀N₈OS
      ReversibleY
      Quality LevelMQ100
      Applications
      Applicationp21-Activated Kinase Inhibitor II, PF-3758309, CAS 898044-15-0, is a cell-permeable, reversible, potent inhibitor of p21-activated kinases (IC50 = 190 and 99 nM against PAK1 and PAK3, respectively).
      Biological Information
      Primary TargetPAK
      Primary Target IC<sub>50</sub>190 and 99 nM for PAK1 and PAK3, respectively)
      Purity≥99% 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 -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      p21-Activated Kinase Inhibitor II, PF-3758309 - CAS 898044-15-0 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Murray, B.W., et al. 2010. Proc. Natl. Acad. Sci. USA. 107, 9446.
      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.

      Revision17-May-2013 JSW
      Synonyms(S)-N-(2-(Dimethylamino)-1-phenylethyl)-6,6-dimethyl-3-(2-methylthieno[3,2-d]pyrimidin-4-ylamino)-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, PAK Inhibitor II, PF3758309
      DescriptionA cell-permeable pyrrolopyrazole that acts as a potent inhibitor against p21-activated kinases (Ki in nM/[ATP] in µM = 13.7/200, 18.7/40, 18.1/80. 17.1/72, respectively, in PAK1, PAK4, PAK5, PAK6 in vitro kinase assays; IC50 = 190 and 99 nM against PAK1 and PAK3, respectively) and potently inhibits cellular PAK4-mediated GEF-H1 Ser810 phosphoryation (IC50 = 1.3 nM using HEK293-derived TR-293-KDG cells) by directly targeting the kinase ATP-binding site in a reversible manner (Kd = 4.5 nM; koff = 0.010/s; t1/2 = 68 s; by SPR using rhPAK4300-591 kinase domain). PF-3758309 is expected to inhibit cellular AMPK and RSK2 activity only at much higher concentrations (estimated IC50 = 40 nM and 171 nM, respectively, assuming cellular [ATP] = 2 mM) and exhibit even less potency toward 144 other cellular kinases when administered at effective concentration range for cellular PAK1/4/5/6 inhibition. In addition to inhibiting PAK4-dependent cellular signaling (IC50 = 24.2 nM against 20 ng/mL TNFα-stimulated NF-κB reporter transcription in HEK293T) and proliferation (IC50 = 0.24 and 27 nM, respectively, against HCT116 and A549 colonies formation) in cultures in vitro, PF-3758309 is also reported to effectively inhibit human tumor growth in nude mice in vivo (% inhibition/tumor/BID p.o. dosage in mg/kg = 97%/HCT116/20, 106%/Colo205/20, 89%/MDA-MB231/20, 71%/A549/10, 85%/M24met/25).
      FormYellowish-white powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number898044-15-0
      Chemical formulaC₂₅H₃₀N₈OS
      Purity≥99% by HPLC
      SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconsitution.
      Storage -20°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
      Toxicity Standard Handling
      ReferencesMurray, B.W., et al. 2010. Proc. Natl. Acad. Sci. USA. 107, 9446.