GSK1838705A
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.
GSK1838705A是小分子激酶抑制剂，能够抑制IGF-1R和胰岛素受体，其IC50分别为2.0和1.6 nM。
IGF-1R是一种跨膜受体，受胰岛素样生长因子1和相关激素IGF-2激活。IGF-1R在调节发育的过程中起重要作用。胰岛素受体也是一种跨膜受体，受胰岛素、IGF-1和IGF-2激活。此受体参与胰岛素信号通路，在调节葡萄糖体内平衡中发挥重要租用。
GSK1838705A 抑制源于血液恶性肿瘤的细胞系的体外扩增，包括大多数骨髓瘤和尤文氏肉瘤，并阻碍体内人肿瘤异种移植物的发展。尽管GSK1838705A抑制胰岛素受体，其在有效剂量下对葡萄糖体内稳态的影响微乎其微。GSK1838705A抑制间变性淋巴瘤激酶（ALK），而ALK迫使间变性大细胞淋巴瘤、一些神经母细胞瘤和一系列非小细胞肺癌的生长扭曲发展。
GSK1838705A抑制ALK，其IC50值为0.5 nM，同时也引起极限忍受剂量下体内ALK逃避肿瘤的完全复发。GSK1838705A作为一种有希望的抗肿瘤制剂有助于人类的发展。
参考文献：
[1]. Sabbatini P, et al. GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers. Mol Cancer Ther. 2009 Oct;8(10):2811-20.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 532.57 |
| Cas No. | 1116235-97-2 |
| Formula | C27H29FN8O3 |
| Solubility | ≥26.65 mg/mL in DMSO; insoluble in H2O; ≥2.4 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | 2-[[2-[[1-[2-(dimethylamino)acetyl]-5-methoxy-2,3-dihydroindol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methylbenzamide |
| SDF | Download SDF |
| Canonical SMILES | CNC(=O)C1=C(C=CC=C1F)NC2=NC(=NC3=C2C=CN3)NC4=C(C=C5CCN(C5=C4)C(=O)CN(C)C)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 | GSK1838705A是IGF-1R、IR 和 ALK的高效抑制剂，其IC50分别为2.0 nM、1.6 nM和0.5 nM。 | |||||
| 靶点 | ALK | Insulin Receptor | IGF-1R | RSK1 | JNK3 | |
| IC50 | 0.5 nM | 1.6 nM | 2 nM | 1.6 μM | 2 μM | |
质量控制和MSDS
- 批次:
化学结构
