Product Name:  GSK1838705A  Request GSK1838705A
CAT#: A-1800    

Chemical Structure

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Biological Activity

GSK1838705A is a small-molecule kinase inhibitor that inhibits IGF-IR and IR (insulin receptor) with IC50s of 2.0 and 1.6 nM, respectively. GSK1838705A blocks the in vitro proliferation of cell lines derived from solid and hematologic malignancies, including multiple myeloma and Ewing's sarcoma, and retards the growth of human tumor xenografts in vivo. Despite the inhibitory effect of GSK1838705A on insulin receptor, minimal effects on glucose homeostasis were observed at efficacious doses. GSK1838705A also inhibits the anaplastic lymphoma kinase (ALK), which drives the aberrant growth of anaplastic large-cell lymphomas, some neuroblastomas, and a subset of non-small cell lung cancers. GSK1838705A inhibits ALK, with an IC(50) of 0.5 nmol/L, and causes complete regression of ALK-dependent tumors in vivo at well-tolerated doses. GSK1838705A is therefore a promising antitumor agent for therapeutic use in human cancers. (source: Mol Cancer Ther. 2009 Oct;8(10):2811-20.).
Technical Data

IUPAC/Chemical name: 2-((2-((1-(2-(dimethylamino)acetyl)-5-methoxyindolin-6-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-6-fluoro-N-methylbenzamide
Chemical Formula: C27H29FN8O3
CAS#: 1116235-97-2
M.Wt: 532.57
Purity: >99%
Storage Conditions: 2ºC to 8 ºC, or -20ºC for 3 years.
Reference