5.38244

Cyclorasin 9A5

• Synonim(y): Cyclorasin 9A5, Cyclic Ras Inhibitor
• Wzór empiryczny (zapis Hilla): C₇₅H₁₀₈FN₂₅O₁₃
• Masa cząsteczkowa: 1586.82
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Próba: ≥98% (HPLC)
• Poziom jakości: 100
• Formularz: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; desiccated (hygroscopic); protect from light
• kolor: off-white
• rozpuszczalność: water: 100 mg/mL
• temp. przechowywania: −20°C

Opis

Opis ogólny

A 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

A 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.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
Ras-GTP

Reversible: yes

Target IC₅₀: 120 nM for K-Ras G12V

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Sekwencja

cyclo(-Trp-Thr-ala-Arg-Arg-Arg-nal-Arg-Fpa-nle-Gln)

Postać fizyczna

Supplied as a trifluoroacetate salt.

Rekonstytucja

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Inne uwagi

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

Informacje prawne

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 1
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable