Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lenalidomide (CC-5013) 是 Thalidomide 的衍生物,也是具有口服活性免疫调节剂,以分子胶的方式作用。它是泛素 E3 连接酶 cereblon (CRBN) 的配体,可通过 CRBN-CRL4 泛素连接酶对两种淋巴转录因子 IKZF1 和 IKZF3 进行选择性泛素化和降解。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 112 | 现货 | ||
5 mg | ¥ 226 | 现货 | ||
10 mg | ¥ 318 | 现货 | ||
25 mg | ¥ 518 | 现货 | ||
50 mg | ¥ 759 | 现货 | ||
100 mg | ¥ 1,120 | 现货 | ||
200 mg | ¥ 1,320 | 现货 | ||
500 mg | ¥ 1,630 | 现货 | ||
1 g | ¥ 2,450 | 现货 | ||
5 g | ¥ 4,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 245 | 现货 |
产品描述 | Lenalidomide (CC-5013) is a potent inhibitor of TNF-α that, at 10 μM, alters gene expression and cell viability in a range of cancer cell lines. |
靶点活性 | TNF-α:13 nM |
体外活性 | Lenalidomide significantly inhibited the proliferation of NSCLC cells (Lu-99, H1299, H460 and A549) in a concentration-dependent manner. In particular, H460 cells had the highest sensitivity for lenalidomide. 3-fold more mRNAs were downregulated (474 mRNAs) than upregulated (158 mRNAs) by lenalidomide (10 μM) treatment in H460 cells [1]. The ubiquitously expressed E3 ligase protein cereblon (CRBN) mediated antiproliferative activities of lenalidomide in myeloma cells, as well as lenalidomide-induced cytokine production in T cells. Lenalidomide inhibited autoubiquitination of CRBN in HEK293T cells expressing thalidomide-binding competent wild-type CRBN, but not thalidomide-binding defective CRBN(YW/AA) [2]. |
体内活性 | Doses of 15 mg/kg IV, 22.5 mg/kg IP, and 45 mg/kg PO lenalidomide caused no observable toxicity up to 24 h postdose. Administration of 0.5 and 10 mg/kg resulted in systemic bioavailability ranges of 90-105% and 60-75% via IP and oral routes, respectively. Lenalidomide was detectable in the brain only after IV dosing of 5 and 10 mg/kg [3]. Oral administration of lenalidomide attenuates growth factor-induced angiogenesis in vivo; the rat mesenteric window assay was utilized to show that lenalidomide significantly inhibits vascularization in a dose-dependent manner [4]. |
细胞实验 | The human NSCLC cell lines Lu-99, H1299, A549, EBC1, and H460 were cultured in RPMI-1640 medium containing 10% fetal bovine serum and antibiotics at 37°C in a humidified chamber containing 5% CO2. Cells were seeded into 60-mm culture dishes (2x10^5 cells per dish) with various concentrations of lenalidomide and incubated for various times [1]. |
动物实验 | Mice were administered sterile preparations of lenalidomide normalized to body weight. Intravenously (IV) dosed animals received drug by bolus tail vein injections, and extravascularly dosed mice received drug by bolus intraperitoneal injections (IP) or oral gavage (PO). Dosing solution, concentrations were adjusted so dose volumes ranged between approximately 100 and 150 μL for IV injections and between approximately 150 and 250 μL for IP and PO dosing in the pharmacokinetic study. However, for the range-finding study, increased dose volumes were used (up to 200 μL IV, 300 μL IP, and 600 μL PO, per approved animal use protocol) to explore elevated lenalidomide doses. The bolus injection rates for all IV, IP, or PO injections were less than 5 s. Concentrations of dosing solutions were verified by liquid chromatography-mass spectrometry [4]. |
别名 | 来那度胺, CC-5013 |
分子量 | 259.26 |
分子式 | C13H13N3O3 |
CAS No. | 191732-72-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (192.86 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.8571 mL | 19.2857 mL | 38.5713 mL | 96.4283 mL |
5 mM | 0.7714 mL | 3.8571 mL | 7.7143 mL | 19.2857 mL | |
10 mM | 0.3857 mL | 1.9286 mL | 3.8571 mL | 9.6428 mL | |
20 mM | 0.1929 mL | 0.9643 mL | 1.9286 mL | 4.8214 mL | |
50 mM | 0.0771 mL | 0.3857 mL | 0.7714 mL | 1.9286 mL | |
100 mM | 0.0386 mL | 0.1929 mL | 0.3857 mL | 0.9643 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。
Lenalidomide 191732-72-6 Apoptosis PROTAC TNF Ligand for E3 Ligase Molecular Glues myeloma Inhibitor CRL4 ligase IKZF1 Ligands for E3 Ligase E3 ligase-recruiting Moiety immunomodulatory cereblon analog multiple CC5013 inhibit ligand CC 5013 IKZF3 来那度胺 degradation CC-5013 inhibitor