Pomalidomide
- 价格： ￥100/支
- 发布日期： 2022-11-09
- 更新日期： 2024-04-28
产品详请
| 产地 |
China
|
| 品牌 |
Chemstan
|
| 货号 |
CSJY002
|
| 用途范围 |
Research Grade
|
| 纯度 |
>98%%
|
| CAS编号 |
19171-19-8
|
| 规格 |
1g
|
| 是否进口 |
否
|
中文名称:泊马度胺
CAS No:19171-19-8
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.
体外活性
Pomalidomide (CC-4047) was significant inhibition against TNFα in Human PBMC cell with an IC50 of 13 nM [1]. Pomalidomide inhibits IL-2-mediated generation of FOXP3 positive CTLA-4 positive CD25high CD4+ T regulatory cells from PBMCs by up to 50% [2]. Exposure of lymphoma cells to CC-4047 resulted in a lesser degree of growth inhibition. Induction of apoptosis was shown in 10% to 26% of lymphoma cells 24 hours following exposure to CC-4047 [3].
体内活性
In vivo studies in severe combined immunodeficient mice showed synergistic activity between CC-4047 plus rituximab. Animals treated with the CC-4047/rituximab combination had a median survival of 74 days [3]. POM has desirable pharmacokinetic properties in the rat. It had relatively slow clearance (12.3 mL/min/kg), a reasonable volume of distribution (1.75 L/kg), and an acceptable bioavailability (47.4%). Following a 50 mg/kg PO administration of POM to rats, unbound concentrations in blood reached a Cmax value of 1100 ± 82 ng/mL at 4.6 ± 2.4 hours, with a concomitant AUC(0?10) value of 6800 ± 2000 ng·hr/mL [4].
激酶实验
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 IC50 is calculated by nonlinear regression analysis [1].
细胞实验
In vitro effects of either CC-5013 or CC-4047 as single agent or in combination with rituximab were evaluated by flow cytometric analysis. Lymphoma cell lines (1 × 10^6 cells) were exposed to either CC-5013 (5 μg/mL), CC-4047 (5 μg/mL), or vehicle control (DMRIE-C, 0.01%) alone or in combination with rituximab at a final concentration of 10 μg/mL. Following a period of incubation of 24 or 48 hou
分子式C13H11N3O4
分子量273.248
参考文献[1]Galustian C, et al. The anti-cancer agents lenalidomide and pomalidomide inhibit the proliferation and function of T regulatory cells. Cancer Immunol Immunother. 2009 Jul;58(7):1033-45.
Note
For research use only .
