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

500613
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₅H₃₀N₈OS 898044-15-0

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      5.00613.0001
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          Glass bottle 5 mg
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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®
          SynonymsPAK Inhibitor II, PF3758309, (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
          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
          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

          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
          SynonymsPAK Inhibitor II, PF3758309, (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
          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.