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GSK1838705A

In stock
Catalog No.
A8440
IGF-IR/IR/ALK inhibitor, ATP-competitive
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$176.00
In stock
5mg
$120.00
In stock
50mg
$680.00
In stock
200mg
$1,540.00
In stock

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Background

GSK1838705A is a small-molecule kinase inhibitor that inhibits IGF-IR and the insulin receptor with IC50s of 2.0 and 1.6 nmol/L, respectively.

IGF-1R is a transmembrane receptor which is activated by insulin-like growth factor 1 and by a related hormone IGF-2. This protein plays important role in the regulation of development. The insulin receptor is also a transmembrane receptor that is activated by insulin, IGF-1 and IGF2. This receptor is involved in insulin signaling pathway and plays an essential role in the regulation of glucose homeostasis.

GSK1838705A obstructs the in vitro expansion of cell lines got from strong and hematologic malignancies, including numerous myeloma and Ewing's sarcoma, and hinders the development of human tumor xenografts in vivo. In spite of the inhibitory impact of GSK1838705A on insulin receptor, insignificant effects on glucose homeostasis were seen at efficacious dosages. GSK1838705A represses the anaplastic lymphoma kinase (ALK), which drives the distorted development of anaplastic substantial cell lymphomas, some neuroblastomas, and a subset of non–small cell lung growths.

GSK1838705A restrains ALK, with an IC50 value of 0.5 nM, furthermore, causes complete relapse of ALK-ward tumors in vivo at very-endured measurements. GSK1838705A arrives for a promising antitumor agent for helpful use in human growth.

Reference:
[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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt532.57
Cas No.1116235-97-2
FormulaC27H29FN8O3
Solubility≥26.65mg/mL in DMSO
Chemical Name2-[[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
SDFDownload SDF
Canonical SMILESCNC(=O)C1=C(C=CC=C1F)NC2=NC(=NC3=C2C=CN3)NC4=C(C=C5CCN(C5=C4)C(=O)CN(C)C)OC
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description GSK1838705A is a potent inhibitor of IGF-1R,IR and ALK with IC50 values of 2.0 nM, 1.6 nM and 0.5 nM, respectively.
Targets ALK Insulin Receptor IGF-1R RSK1 JNK3  
IC50 0.5 nM 1.6 nM 2 nM 1.6 μM 2 μM  

Quality Control

Quality Control & MSDS

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Chemical structure

GSK1838705A