LB100

CAS号

1632032-53-1

分子式

C13H20N2O4

主要靶点

Phosphatase

仅限科研使用

Cat No : CM05904

Print datasheet

Synonyms

PP2A|LB 100|LB100|LB-100



产品信息

CAS号 1632032-53-1
分子式 C13H20N2O4
主要靶点 Phosphatase
主要通路 代谢
分子量 268.31
纯度 98.63%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 PP2A|LB 100|LB100|LB-100

靶点活性

PP2A(Panc-1):3.87 μM|PP2A(BxPc-3):0.85 μM

体内活性

与对照组相比,LB-100使细胞内阿霉素浓度升高约2.5倍,并增加肿瘤细胞对阿霉素的敏感性。LB-100使血管内皮生长因子分泌增加,从而促进HIF-1α-VEGF介导的血管生成。LB-100对BxPc-3(IC50:2.3 μM)和Panc-1(IC50:1.7 μM)细胞的生长有明显抑制效果。经LB-100处理后,BxPc-3、SW1990和Panc-1细胞肿的PP2A活性下降30-50%。

体外活性

在胰腺癌异种移植小鼠模型中, LB-100(2 mg/kg,i.p.)可增加化疗药物阿霉素的疗效.LB-100使肿瘤表面血流速度和肿瘤微血管密度增加.

溶解度

Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:49 mg/mL (182.6 mM);DMSO:< 1 mg/mL (insoluble or slightly soluble)

细胞实验

Cytotoxicity is conducted by using a Cell Counting Kit-8. Cells are seeded in 96-well plates with a density of 3000 cells per well and are assessed after treatments following the CCK-8 protocol. Relative cytotoxicity is expressed as a percentage of speci?c controls. (Only for Reference)

参考文献

1.Bai X, et al. Inhibition of protein phosphatase 2A sensitizes pancreatic cancer to chemotherapy by increasing drug perfusion via HIF-1α-VEGF mediated angiogenesis. Cancer Lett. 2014 Oct 7. pii: S0304-3835(14)00589-8.
2.Bai XL, et al. Inhibition of protein phosphatase 2A enhances cytotoxicity and accessibility of chemotherapeutic drugs to hepatocellular carcinomas. Mol Cancer Ther. 2014 Aug;13(8):2062-72.
3.Fu QH, et al. LB-100 sensitizes hepatocellular carcinoma cells to the effects of sorafenib during hypoxia by activation of Smad3 phosphorylation. Tumour Biol. 2016 Jun;37(6):7277-8

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