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Pomalidomide
物品单位 价格 品牌
100 Chemstan
  • 产地:China
  • 型号:1g
  • 货号:CSJY002
  • cas:19171-19-8
  • 发布日期: 2022-11-09
  • 更新日期: 2022-11-09
产品详细说明
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

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 .




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