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508340 InSolution™ PERK Inhibitor I, GSK2606414 - CAS 1337531-89-1 - Calbiochem

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Synonymes: 1-(5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone, 7-Methyl-5-(1-((3-trifluoromethyl)phenyl)acetyl)-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine

Primary Target: PERK
508340
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Tableau de caractéristiques principal

CAS #Empirical Formula
1337531-89-1C₂₄H₂₀F₃N₅O

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      Description
      Catalogue Number508340
      Brand Family Calbiochem®
      Synonyms1-(5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone, 7-Methyl-5-(1-((3-trifluoromethyl)phenyl)acetyl)-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
      References
      ReferencesAxten, J.M., et al. 2012. J. Med. Chem. 55, 7193.
      Product Information
      CAS number1337531-89-1
      FormLiquid
      FormulationA 25 mM (2 mg/177 µL) sterile-filtered solution of PERK Inhibitor I, GSK2606414 (Cat. No. 516535) in DMSO.
      Hill FormulaC₂₄H₂₀F₃N₅O
      Chemical formulaC₂₄H₂₀F₃N₅O
      Hygroscopic Hygroscopic
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPERK
      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 Dry Ice Only
      Toxicity Standard Handling
      Storage ≤ -70°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Avoid freeze/thaw Avoid freeze/thaw
      Do not freeze Ok to freeze
      Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C. Use only fresh DMSO for further dilutions.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      5083400001 04055977261912

      Documentation

      Références bibliographiques

      Aperçu de la référence bibliographique
      Axten, J.M., et al. 2012. J. Med. Chem. 55, 7193.
      Fiche technique

      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.

      Revision13-December-2013 JSW
      Synonyms1-(5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone, 7-Methyl-5-(1-((3-trifluoromethyl)phenyl)acetyl)-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
      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.
      FormLiquid
      FormulationA 25 mM (2 mg/177 µL) sterile-filtered solution of PERK Inhibitor I, GSK2606414 (Cat. No. 516535) in DMSO.
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1337531-89-1
      Chemical formulaC₂₄H₂₀F₃N₅O
      Structure formulaStructure formula
      Purity≥98% by HPLC
      Storage Protect from light
      Avoid freeze/thaw
      ≤ -70°C
      Hygroscopic
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C. Use only fresh DMSO for further dilutions.
      Toxicity Standard Handling
      ReferencesAxten, J.M., et al. 2012. J. Med. Chem. 55, 7193.