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经验配方 CAS号 C₁₈H₁₇ClO₆ 12772-57-5 描述 概述 A cell-permeable, ATP-site binding, and irreversible antifungal macrocyclic lactone antibiotic that acts as a protein tyrosine kinase inhibitor. Inhibits p60v-src kinase activity (IC50 = 0.27 nM). Inhibits the expression of COX-2 (IC50 = 27 nM) without affecting COX-1 expression in LPS-stimulated macrophages. Disrupts K-Ras-activated signaling pathways by selectively depleting Raf kinase. Inhibits tyrosine phosphorylation of p53/56lyn in LPS-stimulated macrophages. Suppresses NIH/3T3 cell transformation by diverse oncogenes such as src, ras, and mos in part by blocking the key signal transduction intermediates such as MAP kinase and GAP-associated p62. Also exhibits anti-angiogenic activity in vivo. Inhibits Wnt-5A expression in dermal papilla cells (IC50 = 190 nM). 产品目录编号 553400 品牌系列 Calbiochem®
参考 参考 Shinonaga, H., et al. 2009. Bioorg. Med. Chem. 17, In press.
Soga, S., et al. 1998. J. Biol. Chem. 273, 822.
Chanmugam, P., et al. 1995. J. Biol. Chem. 270, 5418.
Shimada, Y., et al. 1995. J. Antibiot. 48, 824.
Zhao, J.F., et al. 1995. Oncogene 11, 161.
Oikawa, T., et al. 1993. Eur. J. Pharmacol. 241, 221.
Kwon, H.J., et al. 1992. Cancer Res. 52, 6926.产品信息 CAS号 12772-57-5 形式 White solid Hill配方 C₁₈H₁₇ClO₆ 化学配方 C₁₈H₁₇ClO₆ Molar Mass 364.8 结构配方图像 生物信息 主靶 p60v-src kinase activity 主靶IC50 0.27 nM 副靶 COX-2 (IC₅₀ = 27 nM) 纯度 ≥98% by HPLC 理化信息 溶解度 DMSO or MeOH GHS安全信息 RTECS RR1105000 安全信息 R相 R: 20/21/22-36/37/38
Harmful by inhalation, in contact with skin and if swallowed.
Irritating to eyes, respiratory system and skin.S相 S: 26-36
In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.
Wear suitable protective clothing.储存和货运信息 货运代码 Ambient Temperature Only
毒性 Harmful
储存 +2°C to +8°C
避光 Protect from light
无需冷冻 No
特殊指南 Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C. 包装信息 惰性气体下包装 Packaged under inert gas
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