Description
GW-441756 (504433-23-2) is a potent and selective TrkA kinase inhibitor (IC50 = 2 nM).
Uses
GW 441756 is an effective Trk binder, a novel bioactive molecule used in the treatment of neuroblastoma in infants.
Definition
ChEBI: 3-[(1-methyl-3-indolyl)methylidene]-1H-pyrrolo[3,2-b]pyridin-2-one is a member of indoles.
Biological Activity
Potent, selective inhibitor of the NGF receptor tyrosine kinase A (TrkA) (IC 50 = 2 nM). Displays > 100-fold selectivity over a range of other kinases.
References
[1] EDGAR R. WOOD. Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles[J]. Bioorganic & Medicinal Chemistry Letters, 2004, 14 4: Pages 953-957. DOI:
10.1016/j.bmcl.2003.12.002[2] TAKUYA TAKEMOTO. Neuroprotection elicited by nerve growth factor and brain-derived neurotrophic factor released from astrocytes in response to methylmercury[J]. Environmental toxicology and pharmacology, 2015, 40 1: Pages 199-205. DOI:
10.1016/j.etap.2015.06.010
