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538092 K-Ras Inhibitor, SAH-SOS1A - Calbiochem

538092
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₀₀H₁₅₉N₂₇O₂₈

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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
      Quality LevelMQ100
      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.