Rapamycin 是一种特异性的 mTOR 抑制剂，IC50 为 0.1 nM。 抗真菌剂和免疫抑制剂。选择性抑制哺乳动物雷帕霉素靶蛋白(mTOR)，并阻断随后的p70 S6激酶激活(IC50 = 50 pM)。可特异性抑制mTORC1，但可磷酸化Akt（蛋白激酶B）Ser473位的mTORC2则对雷帕霉素不敏感。防止 IGF-II 的翻译激活。还防止静止的T细胞进入细胞周期，但不直接阻止细胞周期进程。研究表明，可抑制随后的信号传导事件，例如p110Rb 磷酸化、p34cdc2激酶激活和细胞周期蛋白A合成。表现出与FK-50 6结合蛋白的强结合力。还据报道在鼠B细胞系中诱导凋亡，抑制淋巴因子诱导的细胞增殖（在G1期），并不可逆地阻滞酿酒酵母细胞（在G1）。 Anti-fungal and immunosuppressant. Selectively inhibits the mammalian target of rapamycin (mTOR) and blocks the subsequent activation of p70 S6 kinase (IC50 = 50 pM). Specifically inhibits mTORC1, but mTORC2 that phosphorylates Akt at Ser473 appears to be insensitive to rapamycin. Prevents the translational activation of IGF-II. Also prevents resting T-cells from entering the cell cycle, but does not directly arrest cell cycle progression. Shown to inhibit later signaling events, such as p110Rb phosphorylation, p34cdc2 kinase activation, and cyclin A synthesis. Exhibits strong binding to FK-506 binding proteins. Also reported to induce apoptosis in a murine B-cell line, to inhibit lymphokine-induced cell proliferation at the G1 phase, and to irreversibly arrest Saccharomyces cerevisiae cells in the G1 phase.
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Rapamycin
Dangerous GoodsCAS number：53123-88-9 molecular formula：C51H79NO13
overview
compound introduction
Specs
| Chinese alias | 雷帕霉素 | 西罗莫司 | (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-十六氢-9,27-二羟基-3-[(1R)-2-[(1S,3R,4R)-4-羟基-3-甲氧基环己基]-1-甲基乙基]-10,21-二甲氧基-6,8,12,14,20,26-六甲基-23,27-环氧-3H-吡啶并[2,1-c][1,4]氧杂氮杂环三十一烯-1,5,11,2 | ||
| English alias | AY 22989 | AY-22989 | CHEBI:9168 | EC 610-965-5 | HMS2089A21 | RAPA | (1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-dihydroxy-12-{(2S)-1-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]propan-2-yl}-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl | ||
| CAS number | 53123-88-9 | molecular formula | C51H79NO13 |
| molecular weight | 914.19 g/mol | Exact mass | - |
| PSA | 195.000 Ų | logp | 6 |
numbering system
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physicochemical properties
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Safety information
pictogram：
GHS08
Signal word：
Danger
Hazard Statement：
H351: 怀疑引起遗传缺陷 H372: 通过长时间或反复暴露对器官造成损害 H361: 怀疑破坏生育力或未出生的孩子
Statement of Preventive Measures：
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P203: 使用前，获取、阅读并遵守所有安全说明。 P318: 如果暴露或担心，请就医。 P319: 如果你感到不适，请寻求医疗帮助。
RTECS：
VE6250000
Production methods and uses
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upstream information
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downstream information
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MSDS
Found 1 shareMSDS
53123-88-9 | Rapamycin | Rapamycin from Streptomyces hygroscopicus
