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

508340
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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
      5.08340.0001
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          Glass bottle 2 mg
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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
          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

          Documentation

          References

          Reference overview
          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.

          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 ≤ -70°C
          Hygroscopic
          Protect from light
          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.
          Toxicity Standard Handling
          ReferencesAxten, J.M., et al. 2012. J. Med. Chem. 55, 7193.