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538092 K-Ras Inhibitor, SAH-SOS1A - Calbiochem

K-Ras Inhibitor, SAH-SOS1A - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: K-Ras Inhibitor, SAH-SOS1A

Primary Target: K-Ras
538092
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₀₀H₁₅₉N₂₇O₂₈

Products

Catalogue NumberPackaging Qty/Pack
5.38092.0001 Glass bottle 5 mg
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
Global Trade Item Number
Catalogue Number GTIN
5.38092.0001 04054839119422

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 Protect from light
-20°C
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.
Toxicity Standard Handling
ReferencesLeshchiner, E. S. et al. 2015. Proc. Natl. Acad. Sci. USA. 112, 1761.