Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Pomalidomide (CC-4047) 是一种抗血管生成剂和免疫调节剂,以分子胶的方式作用。它与 E3 连接酶 cereblon 相互作用,诱导必需的 Ikaros 转录因子的降解。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
10 mg | ¥ 429 | 现货 | ||
50 mg | ¥ 644 | 现货 | ||
100 mg | ¥ 831 | 现货 | ||
200 mg | ¥ 918 | 现货 | ||
500 mg | ¥ 996 | 现货 | ||
1 g | ¥ 1,383 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 498 | 现货 |
产品描述 | Pomalidomide (CC-4047) 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:13 nM (PBMCs) |
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 hours, apoptosis was assessed by staining-treated cells with FITC-labeled Annexin V and propidium iodine. All samples were analyzed by multicolor flow cytometric analysis using a fluorescence-activated cell sorter/FACStar Plus flow cytometer. Cells were scored as apoptotic if they were Annexin V–positive and propidium iodine–negative/positive (early and late apoptosis, respectively) [2]. |
动物实验 | These studies were carried out using a disseminated lymphoma-bearing SCID mouse xenograft model. Raji cells were harvested from confluent cultures and only suspensions with >90% viable cells were used for animal inoculation. Subsequently, on day 0, SCID mice received 1 ×10^6 Raji cells via i.v. Untreated SCID mice inoculated by i.v. injection develop symptomatic central nervous system, pulmonary, and liver metastasis that result in death from massive tumor burden and central nervous system involvement after 17 to 21 days after inoculation. A second lymphoma mouse model was used to address the significance of NK cell expansion in the biological interactions observed between rituximab and IMiDs. The second mouse lymphoma xenograft consisted of SCID mice depleted of NK cells bearing Raji cells implanted via tail vein injection as described above [2]. |
别名 | CC-4047, 泊马度胺 |
分子量 | 273.24 |
分子式 | C13H11N3O4 |
CAS No. | 19171-19-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 54 mg/mL (197.63 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.6598 mL | 18.2989 mL | 36.5979 mL | 91.4947 mL |
5 mM | 0.732 mL | 3.6598 mL | 7.3196 mL | 18.2989 mL | |
10 mM | 0.366 mL | 1.8299 mL | 3.6598 mL | 9.1495 mL | |
20 mM | 0.183 mL | 0.9149 mL | 1.8299 mL | 4.5747 mL | |
50 mM | 0.0732 mL | 0.366 mL | 0.732 mL | 1.8299 mL | |
100 mM | 0.0366 mL | 0.183 mL | 0.366 mL | 0.9149 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Pomalidomide 19171-19-8 Apoptosis PROTAC TNF Ligand for E3 Ligase Molecular Glues Ligands for E3 Ligase CC-4047 inhibit 泊马度胺 CC4047 CC 4047 Inhibitor E3 ligase-recruiting Moiety inhibitor