Lenalidomide (CC-5013)是Thalidomide的衍生物，是一种TNF-α分泌抑制剂，IC50为13 nM。Lenalidomide (CC-5013) 是 ubiquitin E3 ligase cereblon (CRBN) 的配体，它通过CRBN-CRL4泛素连接酶引起两个淋巴样转录因子IKZF1和IKZF3的选择性泛素化和降解。Lenalidomide 可促进 cleaved caspase-3 的表达、抑制 VEGF 的表达并诱导凋亡。可用于血液瘤的相关研究。
别名：Revlimid, CC-5013
Lenalidomide (CC-5013)是Thalidomide的衍生物，是一种TNF-α分泌抑制剂，IC50为13 nM。CC-5013强诱导IL-2和sIL-2R产量。CC-5013作用于T细胞，诱导CD28的酪氨酸磷酸化，随后下调NF-κB的激活。 Lenalidomide和Pomalidomide作用于表达与Thalidomide结合野生型CRBN的，而不是Thalidomide结合缺陷型CRBN(YW/AA)的HEK293 T细胞，抑制CRBN自体泛素化。Lenalidomide (CC-5013) 是 ubiquitin E3 ligase cereblon (CRBN) 的配体，它通过CRBN-CRL4泛素连接酶引起两个淋巴样转录因子IKZF1和IKZF3的选择性泛素化和降解。Lenalidomide 可促进 cleaved caspase-3 的表达、抑制 VEGF 的表达并诱导凋亡。可用于血液瘤的相关研究。
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数据来源 | Int Immunopharmacol (2015). Lenalidomide, Figure 9. (AbMole BioScience, Houston, TX, USA) |
| 方法 | MTT assay | |
| 细胞系/动物模型 | BV-2 cells | |
| 浓度 | 10 μM | |
| 处理时间 | 30 min | |
| 实验结果 | Lenalidomide significantly decreased hypoxia-induced mRNA levels of TNF-alpha (Fig. 9A). Next to determine whether the inhibition of TNF-alpha contributes to microglial-CM induced neuron death, BV-2 cells were pretreated with lenalidomide (10 μM) for 30 min, and then exposed hypoxia for 24 h; neuronal cells were treated with different CM from BV-2 cells for 24 h. MTT assay showed that the viability of neurons in the hypoxia-CM condition was significantly decreased, while this effect was reversed by the CM treated with hypoxia and lenalidomide (Fig. 9B). |
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数据来源 | Graduation Thesis (2015) . Figure 14.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2) |
| 方法 | hochest staining and Annexin-V/PI flow cytometry | |
| 细胞系/动物模型 | HL60, MOLM13 and NB4 cells | |
| 浓度 | 1, 5, 20, 50, 100 µM | |
| 处理时间 | 48 h | |
| 实验结果 | An overall higher degree of reduced metabolic activity was observed from three independent studies with MOLM13 (Figure 14A) and NB4 (Figure 14B) cells thus were suggested being more responsive to co-treatment. |
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数据来源 | Graduation Thesis (2015) . Figure 13.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2) |
| 方法 | hochest staining and Annexin-V/PI flow cytometry | |
| 细胞系/动物模型 | HL60, MOLM13 and NB4 cells | |
| 浓度 | 1, 5, 20, 50, 100 µM | |
| 处理时间 | 48 h | |
| 实验结果 | These data indicated a comparable trend of viability in all three cell lines following combinatorial treatment of VPA and LND (Figure 13B, C). HL60 cells are only presented for Hoechst viability scoring in figure 13A since the cells do not expose phosphatidylserine upon apoptosis induction. |
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数据来源 | Graduation Thesis (2015) . Figure 12.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2) |
| 方法 | WST-1 proliferation based assay | |
| 细胞系/动物模型 | HL60 cells | |
| 浓度 | 50, 100 µM | |
| 处理时间 | 48 h | |
| 实验结果 | Maximal potentiation of LND was obtained by 100 µM LND in the sequence VPA→LND+VPA, but no significant increased anti-proliferative effect was obtained from three independent and replicable studies. |
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数据来源 | Graduation Thesis (2015) . Figure 11.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2) |
| 方法 | Hochest staining | |
| 细胞系/动物模型 | HL60, MOLM13 and NB4 cells | |
| 浓度 | 1 µM ~ 500 µM | |
| 处理时间 | 24 h and 48 h | |
| 实验结果 | The frequencies of abnormal nucleic morphology were minor at concentrations lower than 50 µM in all three cell lines. |
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数据来源 | Graduation Thesis (2015) . Figure 10.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2) |
| 方法 | WST-1 proliferation based assay | |
| 细胞系/动物模型 | HL60, MOLM13 and NB4 cells | |
| 浓度 | 20 µM ~ 500 µM | |
| 处理时间 | 48 h | |
| 实验结果 | The IC50 of LND in NB4 (201 µM), HL60 (248 µM) and MOLM13 (124 µM) are presented in Figure 10 B, C and D indicating LND to be more effective after 48 hour treatment in MOLM13 and NB4 cells at lower concentrations than when treated for 24 hours. |
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数据来源 | Graduation Thesis (2015) . Figure 9.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2) |
| 方法 | WST-1 proliferation based assay | |
| 细胞系/动物模型 | HL60, MOLM13 and NB4 cells | |
| 浓度 | HL60 (149 µM, CI: 110-200 µM), MOLM13 (218 µM, CI: 153 – 311 µM), and NB4 (203µM, CI: 106 – 387 µM) | |
| 处理时间 | 24 h | |
| 实验结果 | IC50s of LND was obtained from WST-1 proliferation assay, and are presented in Figure 9B, C and D for HL60 (149 µM), MOLM13 (218 µM) and NB4 (203 µM), respectively. |
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数据来源 | Graduation Thesis (2015) . Figure 7.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2) |
| 方法 | WST-1 proliferation based assay | |
| 细胞系/动物模型 | NB4 cells | |
| 浓度 | 12.5, 25, 50, 75, 100 µ M | |
| 处理时间 | 48 h | |
| 实验结果 | the combination of LND and MMF neither showed significant enhanced potentiation of MMF nor LND. |
| 体外实验* | |
|---|---|
| 细胞系 | HL60, MOLM13 and NB4 cells |
| 方法 | Spectrophotometric quantification of cell proliferation was assayed by the water soluble tetrazolium salt-1 (WST-1) (Roche Ltd, Basel, Switzerland) based colorimetric assay. This tetrazolium salt is reduced extracellularly to formazan dye by enzymes of the plasma membrane oxidoreductase. (122) The primary reductant is NADH derived from the TCA of the mitochondria. Hence, WST-1 is converted by metabolically active cells and was employed to measure cell proliferation. The cell lines HL60, MOLM13 and NB4 were plated in triplicate (20×103 cells/well) in a 96-well microplate and treated with either LND (1, 5, 20, 50, 100, 200, and 500 µM) . |
| 浓度 | 1, 5, 20, 50, 100, 200, and 500 µM |
| 处理时间 | 48 h |
*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。
| 体内实验* | |
|---|---|
| 动物模型 | NOD/scid/gamma (NSG) mice |
| 配制 | 10% DMSO, 70% PEG300 |
| 剂量 | 50 mg/kg daily |
| 给药处理 | i.p. |
*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。
| 分子量 | 259.26 |
| 分子式 | C13H13N3O3 |
| CAS号 | 191732-72-6 |
| 溶解性（25°C） | DMSO 34 mg/mL |
| 储存条件 |
粉末型式 -20°C 3年；4°C 2年 溶于溶剂 -80°C 6个月；-20°C 1个月 |
| 运输方式 | 冰袋运输，根据产品的不同，可能会有相应调整。 |
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.8571 mL | 19.2857 mL | 38.5713 mL |
| 5 mM | 0.7714 mL | 3.8571 mL | 7.7143 mL |
| 10 mM | 0.3857 mL | 1.9286 mL | 3.8571 mL |
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
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