计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
Moligand™ 级 ,适用于对基线干扰要求严格的色谱和分析工作流程。
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
在色谱分析、有机合成和交叉偶联反应领域已被 90 篇同行评审文献引用。
雷帕霉素是从 吸水链霉菌中分离得到的一种抗真菌抗生素。这种抗生素对所有的 白色念珠菌都有效。它可阻断激活T辅助细胞所需的信号转导通路。Rapamycin 是一种特异性的 mTOR 抑制剂,IC50 为 0.1 nM。
Information
In vitro
Rapamycin inhibits endogenous mTOR activity in HEK293 cells with IC50 of ~0.1 nM, more potently than iRap and AP21967 with IC50 of ~5 nM and ~10 nM, respectively. In Saccharomyces cerevisiae, Rapamycin treatment induces a severe G1/S cell cycle arrest and inhibition of translation initiation to levels below 20% of control. Rapamycin significantly inhibits the cell viability of T98G and U87-MG in a dose-dependent manner with IC50 of 2 nM and 1 μM, respectively, while displaying little activity against U373-MG cells with IC50 of >25 μM despite the similar extent of the inhibition of mTOR signaling. Rapamycin (100 nM) induces G1 arrest and autophagy but not apoptosis in Rapamycin-sensitive U87-MG and T98G cells by inhibiting the function of mTOR.
In vivo
Treatment with Rapamycin in vivo specifically blocks targets known to be downstream of mTOR such as the phosphorylation and activation of p70S6K and the release of inhibition of eIF4E by PHAS-1/4E-BP1, leading to complete blockage of the hypertrophic increases in plantaris muscle weight and fibre size. Short-term Rapamycin treatment, even at the lowest dose of 0.16 mg/kg, produces profound inhibition of p70S6K activity, which correlates with increased tumor cell death and necrosis of the Eker renal tumors. Rapamycin inhibits metastatic tumor growth and angiogenesis in CT-26 xenograft models by reducing the production of VEGF and blockage of VEGF-induced endothelial cell signaling. Rapamycin treatment at 4 mg/kg/day significantly reduces tumor growth of C6 xenografts, and tumor vascular permeability.
Cell Data
cell lines:
Concentrations:Dissolved in DMSO, final concentrations ~25 μM
Incubation Time:72 hours
Powder Purity:≥99%
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
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。