Alectinib
作者：齐岳
发布时间：2023-08-23
09:21:35
点击数：
产品名称：Alectinib
产品描述：
| 产品描述 | CH5424802 is an orally available inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with antineoplastic activity. |
| 靶点活性 | ALK:1.9 nM, ALK (R1275Q):3.5 nM, ALK (F1174L):1 nM |
| 体外活性 | 在小鼠中,CH5424802（20 mg/kg）处理能够抑制生长.CH5424802 (2-20 mg/kg)以剂量依赖的方式抑制STAT3磷酸化. |
| 体内活性 | 在表达EML4-ALK的NCI-H2228NSCLC细胞中,CH5424802防止ALK自磷酸化。 在NCI-H2228球状体细胞中, CH5424802诱导凋亡标记 - 半胱天冬酶-3/7样活化。 在淋巴瘤细胞系KARPAS-299和SR与NPM-ALK中, CH5424802阻断融合蛋白的生长。CH5424802对天然ALK（Ki=0.83 nM）和L1196M（Ki=1.56 nM）都具有显着的抑制效力。 CH5424802抑制KAPRAS-299（IC50=3 nM）,KDR（IC50=1.4 μM）。 |
| 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 | CH5424802, RG-7853, 艾乐替尼, AF-802, AF802 |
| 分子量 | 482.628 |
| 分子式 | C30H34N4O2 |
| CAS No. | 1256580-46-7 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: 2.1 mM
DMSO: 12.4 mM
( < 1 mg/mL refers to the product slightly soluble or insoluble )
联系我们：
邮箱：2519696869@qq.com
QQ: 2519696869
电话：18066853083
微信：18066853083
公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
主营产品：COF、MOF单体系列：三蝶烯衍生物、金刚烷衍生物、四苯甲烷衍生物、peg、上转换、石墨烯、光电材料、点击化学、凝集素、载玻片、蛋白质交联剂、脂质体、蛋白、多肽、氨基酸、糖化学等。
