532729 RIP1 Kinase Inhibitor III - Calbiochem

532729
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₀H₁₃F₄N₅O₂

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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
      Quality LevelMQ100
      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.

      Technical Info

      Title
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      White Paper: Further considerations of antibody validation and usage. (EMD)
      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.