532729 RIP1 Kinase Inhibitor III - Calbiochem

532729
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₀H₁₃F₄N₅O₂

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      5327290001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable, orally available furopyrimidinyl-phenyl urea compound that acts as a potent and reversible inhibitor of receptor interacting protein 1 (RIP1) kinase (IC50 = 63 nM and 13 nM in RIP fluorescence polarization and ADP-Glo kinase assays, respectively). Binds to the ATP-binding pocket of RIP1 kinase with enzyme adopting a DLG-out inactive conformation. Shown to be moderately effective in inhibiting 25 other protein kinases in a screening of 300 kinases by radiolabeled assay, but only at high concentrations (~ 1 µM in the presence of 10 mM ATP). Blocks TNFα-induced necrotic cell death (IC50 = 250 nM in U937 cells) and protects mice from TNFα-induced hypothermic shock when injected 15 min. prior to i.v. administration of TNFα. Displays desirable pharmacokinetic properties with good systemic exposure following an oral dose (AUC= 14 mg/h/ml; Cmax = 1,100 ng/ml at 4 hours).

          Please note that the molecular weight for this compound is batch-specific due to variable water content.
          Catalogue Number532729
          Brand Family Calbiochem®
          Synonyms1-(4-(4-Aminofuro[2,3-d]pyrimidin-5-yl)phenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea, RIP1 Inhibitor III, Receptor-Interacting Protein 1 Inhibitor III
          References
          ReferencesHarris, P.A., et al. 2013. ACS Med. Chem. Lett. 4, 1238.
          Product Information
          FormLight orange powder
          Hill FormulaC₂₀H₁₃F₄N₅O₂
          Chemical formulaC₂₀H₁₃F₄N₅O₂
          ReversibleY
          Applications
          Biological Information
          Primary TargetRIP1 Kinase
          Purity≥98% 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).
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          RIP1 Kinase Inhibitor III - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Harris, P.A., et al. 2013. ACS Med. Chem. Lett. 4, 1238.
          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-April-2015 JSW
          Synonyms1-(4-(4-Aminofuro[2,3-d]pyrimidin-5-yl)phenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea, RIP1 Inhibitor III, Receptor-Interacting Protein 1 Inhibitor III
          DescriptionA cell-permeable furopyrimidinyl-phenyl urea compound that potently inhibits RIP1 kinase activity (IC50 = 13 nM; [ATP] = 50 µM) by targeting RIPK1 ATP-binding pocket in its inactive DLG-out conformation (IC50 = 63 nM in competitive binding assays against 5 nM ATP-site ligand) without affecting RIPK2 or RIPK5 activity even at concentrations as high as 1 µM ([ATP] = 10 µM). Effectively prevents TNFα-induced necroptosis in Z-VAD(OMe)-FMK- (Cat. No. 627610) treated U937 cultures (EC50 = 250 nM) in vitro and is efficacious in protecting mice from body temperature loss (by 77%; 20 mg/kg p.o.) when administered 15 min prior to TNFα i.v. injection in vivo with good oral availability (plasma Cmax = 1100 ng/mL, Tmax = 4 h, AUC = 14 µg·h/mL; 2 mg/kg p.o.). Selectivity profiling in a 300-kinase panel shows significant inhibition against only 25 targets (IC50 <1 µM), notably RET, EPHA7, FLT3, EPHA6, HIPK4, DDR2, FMS, PDGFRa, and TrkC (% inhibition at 1 µM = 97%, 97%, 96%, 92%, 91%, 90%, 86%, 84%, 84%, respectively).
          FormLight orange powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₀H₁₃F₄N₅O₂
          Purity≥98% by HPLC
          SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C).
          Toxicity Standard Handling
          ReferencesHarris, P.A., et al. 2013. ACS Med. Chem. Lett. 4, 1238.