538092 K-Ras Inhibitor, SAH-SOS1A - Calbiochem

538092
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₀₀H₁₅₉N₂₇O₂₈

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.38092.0001
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          Glass bottle 5 mg
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          Description
          OverviewA cell-permeable hydrocarbon-stapled, α-helical peptide that mimics the native son of sevenless 1 (SOS1) helical domain (amino acids 929-944) with additional Arg-Arg tag for better cell permeability. Binds to wild-type and mutant KRAS at the SOS1 binding pocket in a sequence-specific manner and disrupts SOS1/KRAS interaction (EC50 = 79, 61, 103, 129, 140, and 124 nM for wild-type, G12D, G12V, G12C, G12S, and Q61H mutants, respectively) and blocks their nucleotide association. Reported to engage both GDP-KRAS and GTP-KRAS. Shown to impair the viability of cancer cells bearing G12D, G12C, G12V, G12S, G13D, and Q61H mutations (IC50 = 5 - 15 µM). Also diminishes the viability of HeLa and Colo320-HSR cells expressing wild-type KRAS. Inhibits the activity of MEK1/2, ERK1/2, and Akt in Panc10.05 cells treated with epidermal growth factor. Also shown to completely suppress the phosphorylation of Akt and ERK1/2 in Drosophila melanogaster expressing V12 mutant form of RAS85D upon RU486 (Cat. No. 475838) treatment.
          Catalogue Number538092
          Brand Family Calbiochem®
          SynonymsK-Ras Inhibitor, SAH-SOS1A
          References
          ReferencesLeshchiner, E. S. et al. 2015. Proc. Natl. Acad. Sci. USA. 112, 1761.
          Product Information
          FormOff-white solid
          FormulationSupplied as a trifluoroacetate salt.
          Hill FormulaC₁₀₀H₁₅₉N₂₇O₂₈
          Chemical formulaC₁₀₀H₁₅₉N₂₇O₂₈
          Hygroscopic Hygroscopic
          ReversibleY
          Applications
          Biological Information
          Primary TargetK-Ras
          Purity≥95% by HPLC
          Physicochemical Information
          Cell permeableY
          Peptide SequenceAc-RRFFGIXLTNXLKTEEGN (X=(S)-2-(4'-pentenyl)Ala, stapled)
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
          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

          K-Ras Inhibitor, SAH-SOS1A - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Leshchiner, E. S. et al. 2015. Proc. Natl. Acad. Sci. USA. 112, 1761.
          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
          SynonymsK-Ras Inhibitor, SAH-SOS1A
          DescriptionA cell-permeable hydrocarbon-stapled, α-helical peptide that mimics the native son of sevenless 1 (SOS1) helical domain (amino acids 929-944) with additional Arg-Arg tag for better cell permeability. Binds to wild-type and mutant KRAS at the SOS1 binding pocket in a sequence-specific manner and disrupts SOS1/KRAS interaction (EC50 = 79, 61, 103, 129, 140, and 124 nM for wild-type, G12D, G12V, G12C, G12S, and Q61H mutants, respectively) and blocks their nucleotide association. Reported to engage both GDP-KRAS and GTP-KRAS. Shown to impair the viability of cancer cells bearing G12D, G12C, G12V, G12S, G13D, and Q61H mutations (IC50 = 5 - 15 µM). Also diminishes the viability of HeLa and Colo320-HSR cells expressing wild-type KRAS. Inhibits the activity of MEK1/2, ERK1/2, and Akt in Panc10.05 cells treated with epidermal growth factor. Also shown to completely suppress the phosphorylation of Akt and ERK1/2 in Drosophila melanogaster expressing V12 mutant form of RAS85D upon RU486 (Cat. No. 475838) treatment.
          FormOff-white solid
          FormulationSupplied as a trifluoroacetate salt.
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₀₀H₁₅₉N₂₇O₂₈
          Peptide SequenceAc-RRFFGIXLTNXLKTEEGN (X=(S)-2-(4'-pentenyl)Ala, stapled)
          Purity≥95% by HPLC
          SolubilityDMSO (5 mg/ml) or H₂O (5 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
          ReferencesLeshchiner, E. S. et al. 2015. Proc. Natl. Acad. Sci. USA. 112, 1761.