LDK378 dihydrochloride
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.
LDK378是高度有效的间变性淋巴瘤激酶（ALK）（胰岛素受体超家族中的一种受体酪氨酸激酶）抑制剂，其IC50值为200 pM。LDK378也对其它激酶显示出中度到高度的抑制作用，其中，只有3种激酶的IC50值低于100 nM，包括IGF-1R（8 nM）、InsR（7 nM）和STK22D（23 nM）。据以往研究，在转染NPM-ALK融合基因的Ba/F3细胞以及携带NPM-ALK融合基因的Karpas-299人类非霍奇金Ki阳性大细胞淋巴瘤中，LDK378抑制细胞增殖，其IC50值分别为22.8 nM和26 nM。
参考文献：
[1]Chen J, Jiang C, Wang S. LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor. J Med Chem. 2013 Jul 25;56(14):5673-4. doi: 10.1021/jm401005u. Epub 2013 Jul 9.
[2]Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M, Sarkisova Y, Sun F, Steffy A, Pferdekamper AC, Li AG, Joseph SB, Kim Y, Liu B, Tuntland T, Cui X, Gray NS, Steensma R, Wan Y, Jiang J, Chopiuk G, Li J, Gordon WP, Richmond W, Johnson K, Chang J, Groessl T, He YQ, Phimister A, Aycinena A, Lee CC, Bursulaya B, Karanewsky DS, Seidel HM, Harris JL, Michellys PY. Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem. 2013 Jul 25;56(14):5675-90. doi: 10.1021/jm400402q. Epub 2013 Jun 26.
| Storage | Store at -20°C |
| M.Wt | 631.06 |
| Cas No. | 1380575-43-8 |
| Formula | C28H38Cl3N5O3S |
| Synonyms | LDK 378 dihydrochloride;LDK-378 dihydrochloride |
| Solubility | ≥12.38 mg/mL in EtOH with ultrasonic; ≥13.7 mg/mL in H2O; ≥29.65 mg/mL in DMSO |
| Chemical Name | 5-chloro-2-N-(5-methyl-4-piperidin-4-yl-2-propan-2-yloxyphenyl)-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine;dihydrochloride |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl.Cl.Cl |
| 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。 |
质量控制和MSDS
- 批次:
化学结构
