首页ApoptosisTNFPomalidomide
Pomalidomide
编号 T2384     别名: CC-4047
CAS 19171-19-8     分子式 C13H11N3O4     分子量 273.24
靶点: TNF-α;
Pomalidomide inhibits TNF-α release in LPS stimulated human PBMCs (IC50: 13 nM). It is an anti-angiogenic agent and an immunomodulator.
纯度:99.40%
规格 库存 单价 数量
5 mg 上海现货 246.00
10 mg 上海现货 344.00
50 mg 上海现货 524.00
100 mg 上海现货 656.00
200 mg 上海现货 1180.00
1 mL * 10 mM (in DMSO) 上海现货 410.00
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生物活性

产品描述

Pomalidomide inhibits TNF-α release in LPS stimulated human PBMCs (IC50: 13 nM). It is an anti-angiogenic agent and an immunomodulator.

靶点活性

TNF-α,13nM

实验溶液

1% DMSO+30% polyethylene glycol+1% Tween 80: 15 mg/mL

体外活性

6.4 nM-10 μM Pomalidomide可增加人外周血T细胞中IL-2的产生,并且在CD4 +亚群中比CD8 +亚群稍强。Pomalidomide在升高IL-2,IL-5和IL-10水平方面比CC-5013更有效,但在提高IFN-γ水平时仅比CC-5013略强。Pomalidomide以剂量依赖性方式增强SEE和Raji细胞在Jurkat细胞中诱导的AP-1转录活性,在1 μM时最大增强4倍。将Raji细胞暴露于不同浓度的Pomalidomide(2.5-40 μg/ mL)48小时导致细胞增殖和DNA合成的显着降低,与对照组相比降低~40% 。Pomalidomide抑制脂多糖(LPS)刺激人PBMC和人全血中的TNF-α释放,IC50值分别为13 nM和25 nM。Pomalidomide抑制IL-2刺激的T调节细胞,IC50为~1 μM。

体内活性

Pomalidomide与利妥昔单抗联用使小鼠的平均生存期为74天,而CC5013/利妥昔单抗治疗为58天,利妥昔单抗单独治疗为45天。Pomalidomide增强利妥昔单对严重联合免疫缺陷小鼠B细胞淋巴瘤的抗肿瘤作用。Pomalidomide和利妥昔单抗的协同效应可以通过耗尽NK细胞完全消除,这支持以下猜想:NK细胞扩增是Pomalidomide可以增强利妥昔单抗抗肿瘤活性的机制。

激酶实验

Inhibition of TNF-α synthesis: TNF-α inhibitory activity is measured in lipopolysacharide (LPS) stimulated PBMC. Pomalidomide is added to human PBMCs 1 hour prior to the addition of LPS (1 μg/mL) and incubation continued for an additional 18-20 hours. Supernatants are then harvested, and the concentration of TNF-α in the supernatants is determined by ELISA. The concentration of Pomalidomide that inhibits TNF- production by 50% (IC50) is calculated by nonlinear regression analysis. The human whole blood TNF- inhibition assay is run in a similar fashion to the PBMC assay except that heparinized fresh human whole blood is plated directly into microtiter plates.

细胞实验

For assessment of cell apoptosis, Lymphoma cell lines are exposed to Pomalidomide (5 μg/mL) for 24 hours or 48 hours. The cells are stained with FITC-labeled Annexin V and propidium iodine. Cell apoptosis is analyzed by multicolor flow cytometric analysis using a fluorescence-activated cell sorter/FACStar Plus flow cytometer. Cells are scored as apoptotic if they are Annexin V–positive and propidium iodine–negative/positive (early and late apoptosis, respectively). For determination of cell proliferation, the Lymphoma cell lines are exposed to Pomalidomide (2.5, 5, 10, 20, and 40 μg/mL) for 24 hours or 48 hours. 1 μCi per well (96-well plate) of [3H]-thymidine is added and cells are incubated for another 18 hours. Cells are then harvested using the Harvest system into the 96-well glass filters and [3H]-thymidine uptake is measured using an automated scintillation counter.(Only for Reference)

细胞系: Raji, SU-DHL-4 and SU-DHL-10 cell lines

动物实验

动物模型:Disseminated lymphoma-bearing SCID mice

化学信息

分子量

273.24

分子式

C13H11N3O4

CAS

19171-19-8

溶解度

DMSO: 54 mg/mL (197.63 mM)

Water: <1 mg/mL

Ethanol: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 3.66 ml 18.299 ml 36.598 ml
5 mM 0.732 ml 3.66 ml 7.32 ml
10 mM 0.366 ml 1.83 ml 3.66 ml
50 mM 0.073 ml 0.366 ml 0.732 ml
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