538244 Cyclorasin 9A5 - Calbiochem

538244
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₇₅H₁₀₈FN₂₅O₁₃

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.38244.0001
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          Glass bottle 5 mg
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          Description
          OverviewA cell-permeable 11-mer cyclic peptide that displays high-affinity towards Ras-GTP (IC50 = 120 nM for K-Ras G12V) and inhibits Ras signaling. Shown to readily localize into cytoplasm and directly bind to Ras-GTP near the effector-binding site in a reversible manner. Dose-dependently impairs Ras-B-Raf interaction and blocks EGF-stimulated activation of Akt, MEK & ERK (IC50 = 3.1 µM in H1299 cells). Efficiently induces lung cancer cell growth arrest and triggers apoptosis (LD50 = 3.0 µM in H1299). NOTE: ala = D-Alanine; nal = D-2-naphthylalanine; nle = D-norleucine; Fpa = L-4-Fluorophenylalanine

          Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
          Catalogue Number538244
          Brand Family Calbiochem®
          SynonymsCyclic Ras Inhibitor
          References
          ReferencesUpadhyaya. P., et al. 2015. Angew. Chem. Int. Ed. 54, 7602.
          Product Information
          FormOff-white solid
          FormulationSupplied as a trifluoroacetate salt.
          Hill FormulaC₇₅H₁₀₈FN₂₅O₁₃
          Chemical formulaC₇₅H₁₀₈FN₂₅O₁₃
          Hygroscopic Hygroscopic
          ReversibleY
          Applications
          Biological Information
          Primary TargetRas-GTP
          Primary Target IC<sub>50</sub>120 nM for K-Ras G12V
          Purity≥98% by HPLC
          Physicochemical Information
          Cell permeableY
          Peptide Sequencecyclo(-Trp-Thr-ala-Arg-Arg-Arg-nal-Arg-Fpa-nle-Gln)
          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
          Hygroscopic Hygroscopic
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          References

          Reference overview
          Upadhyaya. P., et al. 2015. Angew. Chem. Int. Ed. 54, 7602.
          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.

          Revision28-July-2017 JSW
          SynonymsCyclic Ras Inhibitor
          DescriptionA cell-permeable 11-mer cyclic peptide that displays high-affinity towards Ras-GTP (IC50 = 120 nM for K-Ras G12V) and inhibits Ras signaling. Shown to readily localize into cytoplasm and directly bind to Ras-GTP near the effector-binding site in a reversible manner. Dose-dependently impairs Ras-B-Raf interaction and blocks EGF-stimulated activation of Akt, MEK & ERK (IC50 = 3.1 µM in H1299 cells). Efficiently induces lung cancer cell growth arrest and triggers apoptosis (LD50 = 3.0 µM in H1299). NOTE: ala = D-Alanine; nal = D-2-naphthylalanine; nle = D-norleucine; Fpa = L-4-Fluorophenylalanine
          FormOff-white solid
          FormulationSupplied as a trifluoroacetate salt.
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₇₅H₁₀₈FN₂₅O₁₃
          Peptide Sequencecyclo(-Trp-Thr-ala-Arg-Arg-Arg-nal-Arg-Fpa-nle-Gln)
          Purity≥98% by HPLC
          SolubilityH₂O (100 mg/ml)
          Storage -20°C
          Hygroscopic
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesUpadhyaya. P., et al. 2015. Angew. Chem. Int. Ed. 54, 7602.