516535 PERK Inhibitor I, GSK2606414 - CAS 1337531-89-1 - Calbiochem

516535
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₄H₂₀F₃N₅O 1337531-89-1

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      516535-5MG
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          Glass bottle 5 mg
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          Description
          OverviewA cell-permeable pyrrolopyrimidamine compound that acts as a highly potent EIF2AK3/PERK inhibitor (IC50 = 0.4 nM; [ATP] = 5 µM) by targeting PERK in its inactive DFG conformation at the ATP-binding region, while displaying ≥385-fold selectivity over c-Kit, Aurora B, BRK, HRI/EIF2AK1, MLK2/MAP3K10, c-MER, DDR2, PKR/EIF2AK2, and MLCK2/MYLK2 (IC50 = 154, 407, 412, 420, 452, 474, 524, 696, and 701 nM, respectively) and little activity against more than 280 other kinases (IC50 >1 µM). Shown to block ER stress-induced PERK autophosphorylation following Thapsigargin (Cat. No. 586005) addition in A549 cultures in vitro (by 100% at ≤30 nM; 60 min preincubation) and effectively retard PxBC-3 tumor growth in mice in vivo (50 and 150 mg/kg/12 h p.o.). Also available as a 25 mM solution in DMSO (Cat. No. 508340).
          Catalogue Number516535
          Brand Family Calbiochem®
          SynonymsEIF2AK3 Inhibitor I, PKR Inhibitor II, MERTK Inhibitor II, RP38 Inhibitor II, TAM Family RTK Inhibitor II, Double-stranded RNA-activated Protein Kinase Inhibitor II, Double-stranded RNA-dependent Protein Kinase Inhibitor II, 7-Methyl-5-(1-((3-trifluoromethyl)phenyl)acetyl)-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine, 1-(5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone, DDR2 Inhibitor I, EIF2AK1 Inhibitor I, EIF2AK2 Inhibitor II, HRI Inhibitor I, MLCK Inhibitor VI, MLK2/MAP3K10 Inhibitor I, PKR-like ER Kinase Inhibitor I, Aurora Kinase Inhibitor IX, BRK Inhibitor I, c-Kit Inhibitor III, Mer RTK Inhibitor II
          References
          ReferencesMoreno, J.A., et al. 2013. Sci Transl. Med.<\i> 5, 1.
          Axten, J.M., et al. 2012. J. Med. Chem. 55, 7193.
          Product Information
          CAS number1337531-89-1
          FormWhite powder
          Hill FormulaC₂₄H₂₀F₃N₅O
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          ApplicationPERK Inhibitor I, GSK2606414, CAS 1337531-89-1, is a cell-permeable, highly potent EIF2AK3/PERK inhibitor (IC50 = 0.4 nM) that targets PERK in its inactive DFG conformation at the ATP-binding region.
          Biological Information
          Primary TargetPerk
          Primary Target IC<sub>50</sub>0.4 nM against EIF2AK3/PERK-catalyzed EIF2&alpha
          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 (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          516535

          References

          Reference overview
          Moreno, J.A., et al. 2013. Sci Transl. Med.<\i> 5, 1.
          Axten, J.M., et al. 2012. J. Med. Chem. 55, 7193.
          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-September-2013 JSW
          SynonymsEIF2AK3 Inhibitor I, PKR Inhibitor II, MERTK Inhibitor II, RP38 Inhibitor II, TAM Family RTK Inhibitor II, Double-stranded RNA-activated Protein Kinase Inhibitor II, Double-stranded RNA-dependent Protein Kinase Inhibitor II, 7-Methyl-5-(1-((3-trifluoromethyl)phenyl)acetyl)-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine, 1-(5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone, DDR2 Inhibitor I, EIF2AK1 Inhibitor I, EIF2AK2 Inhibitor II, HRI Inhibitor I, MLCK Inhibitor VI, MLK2/MAP3K10 Inhibitor I, PKR-like ER Kinase Inhibitor I, Aurora Kinase Inhibitor IX, BRK Inhibitor I, c-Kit Inhibitor III, Mer RTK Inhibitor II
          DescriptionA cell-permeable pyrrolopyrimidinamine compound that acts as a highly potent inhibitor against EIF2AK3/PERK-catalyzed EIF2α Ser51 phosphorylation in kinase assays (IC50 = 0.4 nM; 30 min preincubation; [ATP] = 5 µM) as well as ER stress-induced PERK autophosphorylation following Thapsigargin (Cat. No. 586005) addition in A549 cultures (by 100% with ≤30 nM inhibitor; 60 min preincubation) by targeting PERK in its inactive conformation at the ATP-binding region. Displays ≥385-fold selectivity over c-Kit, Aurora B, BRK, HRI/EIF2AK1, MLK2/MAP3K10, c-MER, DDR2, PKR/EIF2AK2, and MLCK2/MYLK2 (IC50 = 154, 407, 412, 420, 452, 474, 524, 696, and 701 nM, respectively) and exhibits much reduced or little activity against more than 280 other kinases (IC50 >1 µM). Reported to be orally available in dog, mouse, and rat with good pharmacokinetics and retard the growth of established PxBC-3 tumor mass in mice in vivo (by 20% and 59% at the end of a 21 day treatment period with b.i.d. oral dosage of 50 and 150 mg/kg, respectively). The preincubation time-dependent inhibition, extremely slow dissociation rate, as well as the observed PERK selectivity, are all consistent with the inhibitor targeting PERK in its inactive DFG conformation.
          FormWhite powder
          Intert gas (Yes/No) Packaged under inert gas
          CAS number1337531-89-1
          Structure formulaStructure formula
          Purity≥99% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage -20°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesMoreno, J.A., et al. 2013. Sci Transl. Med.<\i> 5, 1.
          Axten, J.M., et al. 2012. J. Med. Chem. 55, 7193.