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5.38244

Sigma-Aldrich

Cyclorasin 9A5

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Synonym(s):
Cyclorasin 9A5, Cyclic Ras Inhibitor
Empirical Formula (Hill Notation):
C75H108FN25O13
Molecular Weight:
1586.82

assay

≥98% (HPLC)

Quality Level

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

off-white

solubility

water: 100 mg/mL

storage temp.

−20°C

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This Item
5.380925.3262607-1464
vibrant-m

5.38244

Cyclorasin 9A5

vibrant-m

5.38092

K-Ras Inhibitor, SAH-SOS1A

vibrant-m

5.32626

Ral Activation Inhibitor, BQU57

vibrant-m

07-1464

Anti-Rac1 Antibody

assay

≥98% (HPLC)

assay

≥95% (HPLC)

assay

≥97% (HPLC)

assay

-

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

-

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

−20°C

storage temp.

−20°C

storage temp.

2-8°C

storage temp.

-

solubility

water: 100 mg/mL

solubility

DMSO: 5 mg/mL, water: 5 mg/mL

solubility

DMSO: 50 mg/mL

solubility

-

General description

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.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Ras-GTP
Reversible: yes
Target IC50: 120 nM for K-Ras G12V

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Sequence

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

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

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

Other Notes

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

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable


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