Description
As a small-molecule kinase inhibitor, GSK1838705A can inhibit IGF-IR, the insulin receptor and ALK with IC50 of 2 nM, 1.6 nM and 0.5 nM.
Storage
2 years at -20 centigrade
Targets
IGF-IR, IR(Insulin receptor), ALK
Molecular Formula
C27H29FN8O3
Chemical Name
2-(2-(1-(2-(dimethylamino)acetyl)-5-methoxyindolin-6-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-6-fluoro-N-methylbenzamide
Solubility
DSMO 107 mg/mL Water
In vitro
As a small-molecule kinase inhibitor, GSK1838705A can inhibit IGF-IR and the insulin receptor with IC50 of 2 nM and 1.6 nM. GSK1838705A also inhibits ALK (anaplastic lymphoma kinase), which drives the aberrant growth of anaplastic large-cell lymphomas, some neuroblastomas, and a subset of non-small cell lung cancers, with an IC50 of 0.5 nM.
In vivo
GSK1838705A blocks the in vitro proliferation of cell lines derived from solid and hematologic malignancies, including multiple myeloma and Ewings sarcoma, and retards the growth of human tumor xenografts in vivo. By inhibiting ALK, GSK1838705A can cause complete regression of ALK-dependent tumors.
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