Alectinib
作者：齊岳
發布時間：2023-08-23
09:21:35
點擊數：
產品名稱：Alectinib
產品描述：
| 產品描述 | CH5424802 is an orally available inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with antineoplastic activity. |
| 靶點活性 | ALK:1.9 nM, ALK (R1275Q):3.5 nM, ALK (F1174L):1 nM |
| 體外活性 | 在小鼠中,CH5424802（20 mg/kg）處理能夠抑制腫瘤生長.CH5424802 (2-20 mg/kg)以劑量依賴的方式抑制STAT3磷酸化. |
| 體內活性 | 在表達EML4-ALK的NCI-H2228NSCLC細胞中,CH5424802防止ALK自磷酸化。 在NCI-H2228球狀體細胞中, CH5424802誘導凋亡標記 - 半胱天冬酶-3/7樣活化。 在淋巴瘤細胞系KARPAS-299和SR與NPM-ALK中, CH5424802阻斷融合蛋白的生長。CH5424802對天然ALK（Ki=0.83 nM）和L1196M（Ki=1.56 nM）都具有顯著的抑制效力。 CH5424802抑制KAPRAS-299（IC50=3 nM）,KDR（IC50=1.4 μM）。 |
| 激酶實驗 | 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. |
| 細胞實驗 | 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) |
| 別名 | CH5424802, RG-7853, 艾樂替尼, AF-802, AF802 |
| 分子量 | 482.628 |
| 分子式 | C30H34N4O2 |
| CAS No. | 1256580-46-7 |
存儲
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 )
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西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發，涵蓋生物科技、化學品、中間體和化工材料等領域。
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