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Alectinib (RG-7853) 是一种 ALK 抑制剂 (IC50=1.9 nM,Kd=2.4 nM),具有选择性、口服活性和 ATP 竞争性。Alectinib 具有抗肿瘤活性,被用于非小细胞肺癌的治疗。
Alectinib (RG-7853) 是一种 ALK 抑制剂 (IC50=1.9 nM,Kd=2.4 nM),具有选择性、口服活性和 ATP 竞争性。Alectinib 具有抗肿瘤活性,被用于非小细胞肺癌的治疗。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 293 | In stock | |
2 mg | ¥ 413 | In stock | |
5 mg | ¥ 689 | In stock | |
10 mg | ¥ 868 | In stock | |
25 mg | ¥ 1,390 | In stock | |
50 mg | ¥ 1,990 | In stock | |
100 mg | ¥ 3,180 | In stock | |
200 mg | ¥ 4,570 | In stock |
Alectinib 相关产品
产品描述 | Alectinib (RG-7853) is an ALK inhibitor (IC50=1.9 nM, Kd=2.4 nM) that is selective, orally active, and ATP-competitive. Alectinib has antitumor activity and is used in the treatment of non-small cell lung cancer. |
靶点活性 | ALK:1.9 nM, ALK (F1174L):1 nM, ALK (R1275Q):3.5 nM |
体外活性 | 方法:六种神经母细胞瘤 (NB) 细胞系用 Alectinib (0.001-50 µM) 处理 72 h,通过 CCK-8 assay 检测细胞活力。 |
体内活性 | 方法:为检测体内抗肿瘤活性,将 Alectinib (25 mg/kg) 腹腔注射给 TH-MYCN 转基因小鼠,每两天一次,给药 11 次。 |
激酶实验 | Kinase inhibitory assays in Vitro: The inhibitory ability against each kinase except for MEK1 and Raf-1 is evaluated by examining their ability to phosphorylate various substrate peptides in the presence of CH5424802 using time-resolved fluorescence resonance energy transfer (TR-FRET) assay or fluorescence polarization (FP) assay. The inhibitory activity against MEK1 is evaluated by quantitative analysis of the phosphorylation of a substrate peptide by a recombinant ERK2 protein in the presence of CH5424802. The inhibitory activity against Raf-1 is evaluated by examining the ability of the kinases to phosphorylate MEK1 in the presence of CH5424802. |
细胞实验 | Cells including NSCLC, A549 and HCC827 are seeded in 96-well plates overnight and incubated with various concentrations of CH5424802 for the indicated time. For spheroid cell growth inhibition assay, cells are seeded on spheroid plates, incubated overnight, and then treated with compound for the indicated times. The viable cells are measured by the Luminescent Cell Viability Assay. Caspase-3/7 assay is evaluated using the Caspase-Glo 3/7 Assay Kit.(Only for Reference) |
别名 | 艾乐替尼, 阿来替尼, RG-7853, CH5424802, AF-802, AF802 |
分子量 | 482.62 |
分子式 | C30H34N4O2 |
CAS No. | 1256580-46-7 |
Smiles | CCc1cc2C(=O)c3c([nH]c4cc(ccc34)C#N)C(C)(C)c2cc1N1CCC(CC1)N1CCOCC1 |
密度 | 1.28 |
颜色 | White |
物理性状 | Solid |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
溶解度信息 | H2O: 2.1 mM, Sonication is recommended. DMSO: 4.83 mg/mL (10 mM), Sonication is recommended. ![]() | |||||||||||||||||||||||||
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以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
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