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) Wood et al. (2004) Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles. Bioorg. Med. Chem. Lett. 14 953
2) Takemoto et al. (2015) Neuroprotection elicited by nerve growth factor and brain-derived neurotrophic factor released from astrocytes in response to methylmercury; Environ. Toxicol. Pharmacol. 40 199 [Focus Citation]
