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LB-100

 
Catalog No.
B4846
蛋白磷酸酶2A(PP2A)抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 954.00
现货
25mg
¥ 3,045.00
现货
100mg
¥ 6,354.00
现货

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A

背景

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.

文献引用

化学属性

Physical AppearanceA solid
StorageStore at -20°C
M.Wt268.31
Cas No.1026680-07-8
FormulaC13H20N2O4
Solubility≥26.8 mg/mL in H2O; insoluble in EtOH; insoluble in DMSO
Chemical Name3-(4-methylpiperazine-1-carbonyl)-7-oxabicyclo[2.2.1]heptane-2-carboxylic acid
SDFDownload SDF
Canonical SMILESCN1CCN(C(C(C2CCC3O2)C3C(O)=O)=O)CC1
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试验操作

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 doxorubicin in 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.

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