CAS NO: | 1026680-07-8 |
包装 | 价格(元) |
5mg | 电议 |
25mg | 电议 |
100mg | 电议 |
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 268.31 |
Cas No. | 1026680-07-8 |
Formula | C13H20N2O4 |
Solubility | ≥26.8 mg/mL in H2O; insoluble in EtOH; insoluble in DMSO |
Chemical Name | 3-(4-methylpiperazine-1-carbonyl)-7-oxabicyclo[2.2.1]heptane-2-carboxylic acid |
Canonical SMILES | CN1CCN(C(C(C2CCC3O2)C3C(O)=O)=O)CC1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
LB-100 is an inhibitor of protein phosphatase 2A (PP2A) with anticancer activity, with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells, respectively[1].
In BxPc-3, Panc-1, and SW1990 cells, LB-100 treatment reduced PP2A activity by 30-50%. LB-100 increases the intracellular doxorubicin concentration (about 2.5 times that of the control group) and makes tumor cells more sensitive to the cytotoxicity of doxorubicin[1].
In a PANC-1 mouse xenograft model, LB-100 (2 mg / kg, intraperitoneal injection) improves the efficacy of the chemotherapy drug doxorubicin. LB-100 increases tumor microvessel density and blood flow velocity on the tumor surface, and decreases tumor volume[1].
Reference:
[1]. Bai X, Zhi X, Zhang Q, 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, 355(2): 281-287.
Cell experiment:[1] | |
Cell lines | Pancreatic cancer cell lines BxPc-3 and Panc-1 |
Reaction Conditions | 0.85 and 3.87 μM LB-100 |
Applications | LB-100 showed dose-dependent inhibition of cell growth in both cell lines. The IC50 of LB-100 was 0.85 μM and 3.87 μM in BxPc-3 and Panc-1, respectively. While the IC50 of doxorubicin was 2.3 μM and 1.7 μM in BxPc-3 and Panc-1, respectively, LB-100 did not synergize with doxorubicin in both cell lines. |
Animal experiment:[1] | |
Animal models | BALB/c nude mice bearing Panc-1 xenografts |
Dosage form | 2 mg/kg Injected intraperitoneally (i.p.) on alternate days for a total of 16 days |
Applications | LB-100 synergistically enhanced the activity of doxorubicinin vivo. This effect was associated with increased microvessel density, blood perfusion, and doxorubicin concentrations within the xenografts. |
Note | The technical data provided above is for reference only. |
References: 1. Bai X, Zhi X, Zhang Q, et al. Inhibition of protein phosphatase 2A sensitizes pancreatic cancer to chemotherapy by increasing drug perfusion via HIF-1α-VEGF mediated angiogenesis. Cancer Letters, 2014, 355(2): 281-287. |