GSK1838705A is a pyrrolopyrimidine-based inhibitor of IGF-1R, IR, and ALK with IC50s of 2.0, 1.6, and 0.5 nM, respectively. Despite its potency against the insulin receptor, no major effect on glucose homeostasis was observed at efficacious doses. [1] In NIH-3T3/USN and NIH-3T3-hIR cell lines GSK1838705A inhibits ligand-induced phosphorylation of IGF1R and IR in a concentration-dependent manner, with concomitant decrease in phosphorylated AKT, IRS-1, and ERK. Antiproflierative EC50s ranged from 20 nM to 8 uM, with most values
In IGF-1-induced mice xenografts, a single oral dose of GSK1838705A at 0.1 and 0.3 mg/kg resulted in 35% and 65% inhibition sof IGF-1R phosphorylation; doses >1 mg/kg completely inhibited phosphorylation. [1]

In ALCL tumor cells bearing ALK fusion genes, proliferation was inhibited in a concentration-dependent manner with EC50s ranging from 24 to 88 nM. [1]

Technical information:

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4^oC desiccated, or store DMSO solution at -20^oC.

Reference:

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.