ALK-IN-1
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.
ALK-IN-1是一种新型的、合成的间变性淋巴瘤激酶(ALK)口服小分子抑制剂,IC50(最大半数抑制浓度)范围为5 nmol/l至11 nmol/l,ALK是胰岛素受体超家族的受体酪氨酸激酶。ALK-IN-1也能够抑制ALK酪氨酸激酶突变L1196M,IC50为15 nmol/l 至45 nmol/L、抑制表皮生长因子受体(EGFR)突变体T790M突变和c-ros的癌基因1(ROS1)。而且,ALK-IN-1在含野生型或突变型EML4-ALK的H3122细胞(敏感的和抗性的)和Ba / F3细胞(IC50分别为10 nM和24 nM)中也具有活性。
参考文献:
[1]Solomon B, Wilner KD, Shaw AT. Current status of targeted therapy for anaplastic lymphoma kinase-rearranged non-small cell lung cancer. Clin Pharmacol Ther. 2014 Jan;95(1):15-23. doi: 10.1038/clpt.2013.200. Epub 2013 Oct 3.
[2]Katayama R1, Khan TM, Benes C, Lifshits E, Ebi H, Rivera VM, Shakespeare WC, Iafrate AJ, Engelman JA, Shaw AT. Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc Natl Acad Sci U S A. 2011 May 3;108(18):7535-40. doi: 10.1073/pnas.1019559108. Epub 2011 Apr 18.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 529.01 |
Cas No. | 1197958-12-5 |
Formula | C26H34ClN6O2P |
Synonyms | Brigatinib analog |
Solubility | ≥26.45 mg/mL in DMSO; insoluble in H2O; ≥55.9 mg/mL in EtOH |
Chemical Name | 5-chloro-2-N-[4-[4-(dimethylamino)piperidin-1-yl]-2-methoxyphenyl]-4-N-(2-dimethylphosphorylphenyl)pyrimidine-2,4-diamine |
SDF | Download SDF |
Canonical SMILES | CN(C)C1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC=CC=C4P(=O)(C)C)Cl)OC |
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 | ALK-IN-1 is a potent inhibitor of ALK with IC50 of 0.62 nM. | |||||
Targets | ALK | FER | ROS/ROS1 | FLT3 | FES/FPS | |
IC50 | 0.62 nM | 1.3 nM | 1.9 nM | 2.1 nM | 3.4 nM |