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产品别名
Cyclorasin 9A5-Calbiochem
Cyclic Ras Inhibitor
基本信息
| Empirical Formula【经验(实验)分子式】 | C75H108FN25O13 |
| Molecular weight | 1586.82 |
| General description【一般描述】 | 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【生化/生理作用】 | Cell permeable: yes Target IC50: 120 nM for K-Ras G12V Primary Target Ras-GTP Reversible: yes |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Sequence【序列】 | cyclo(-Trp-Thr-ala-Arg-Arg-Arg-nal-Arg-Fpa-nle-Gln) |
| Physical form【外形】 | Supplied as a trifluoroacetate salt. |
| Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. |
| Other Notes【其他说明】 | Upadhyaya. P., et al. 2015. Angew. Chem. Int. Ed.54, 7602. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze desiccated (hygroscopic) protect from light |
| color【颜色】 | off-white |
| solubility【溶解性】 | water: 100 mg/mL |
| storage temp.【储存温度】 | −20℃ |
| packaging【包装】 | Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 1 |
