CH5424802
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
CH5424802是ALK的强效选择性抑制剂。
间变性淋巴瘤激酶（ALK）是一种在某些癌症中组成型激活的酪氨酸激酶。
体外实验：在无细胞实验中，CH5424802抑制ALK酶活性的IC50值为1.9 nM，从ALK的解离是ATP竞争性的，Kd值为2.4 nM。F1174L和R1275Q是神经母细胞瘤的两个热点激活突变，CH5424802对其抑制活性与野生型ALK相当[1]。
体内实验：在NCI-H2228模型中，CH5424802口服给药可导致剂量依赖性的肿瘤生长抑制和肿瘤消退，ED50为0.46 mg/kg。此外，使用剂量为20 mg/kg的CH5424802治疗，引发快速的肿瘤消退，在为期4周的无药期，没有肿瘤再生长[2]。
临床试验：目前没有可用临床数据。
参考文献：
[1] Sakamoto H, Tsukaguchi T, Hiroshima S, Kodama T, Kobayashi T, Fukami TA, Oikawa N, Tsukuda T, Ishii N, Aoki Y. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011 May 17;19(5):679-90.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 482.62 |
| Cas No. | 1256580-46-7 |
| Formula | C30H34N4O2 |
| Solubility | insoluble in H2O; ≥2.72 mg/mL in EtOH with gentle warming; ≥4.83 mg/mL in DMSO with gentle warming and ultrasonic |
| Chemical Name | 9-ethyl-6,6-dimethyl-8-(4-morpholin-4-ylpiperidin-1-yl)-11-oxo-5H-benzo[b]carbazole-3-carbonitrile |
| SDF | Download SDF |
| Canonical SMILES | CCC1=C(C=C2C(=C1)C(=O)C3=C(C2(C)C)NC4=C3C=CC(=C4)C#N)N5CCC(CC5)N6CCOCC6 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | Alectinib（CH5424802）是ALK的有效抑制剂，IC50值为1.9 nM。 | |||||
| 靶点 | ALK (F1174L) | ALK | ALK (R1275Q) | INSR | KDR | |
| IC50 | 1 nM | 1.9 nM | 3.5 nM | 550 nM | 1.4 μM | |
化学结构
