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GW 441756
- Moderately soluble in DMSO
- MF: C17H13N3O
- MW: 275.3
Description
GW 441756 is a potent and orally active TrkA/NTRK1 kinase inhibitor with a reported IC50 value of 2 nM.
TrkA transduces nerve growth factor (NGF) signals that control neuronal survival, differentiation, pain sensitization and tumor biology. GW 441756 is used to block TrkA-dependent phosphorylation and downstream neurotrophin signaling.
Key Features
- Potent TrkA/NTRK1 kinase inhibitor
- Reported IC50: 2 nM
- Blocks NGF-TrkA signaling
- Relevant to pain, neurotrophin and cancer pathway research
Applications
- TrkA kinase inhibition assays
- NGF signaling studies
- Pain sensitization pathway research
- Neurotrophin-dependent survival and differentiation models
More Information
| Parent CAS No. | 504433-23-2 |
|---|---|
| Chemical Name | 3-[1-(1-Methyl-1H-indol-3-yl)-meth-(Z)-ylidene]-1,3-dihydro-pyrrolo[3,2-b]pyridin-2-one |
| SMILES | N1(C)C=C(/C=C2C(=O)NC3=CC=CN=C32)C2C=CC=CC=21 |
| MFCD | MFCD08703104 |
| InChi | InChI=1S/C17H13N3O/c1-20-10-11(12-5-2-3-7-15(12)20)9-13-16-14(19-17(13)21)6-4-8-18-16/h2-10H,1H3,(H,19,21)/b13-9- |
| InChiKey | NXNQLECPAXXYTR-LCYFTJDESA-N |
| CID | 9943465 |
| Short Description | TrkA inhibitor |
References
- ER Wood et al. Discovery and in vitro evaluation of potent TrkA kinase inhibitors: Oxindole and aza-oxindoles. Bioorg. Med. Chem. Lett. 2004, 14(4), 953-957.
- J Wang et al. Cellular Assays for High-Throughput Screening for Modulators of Trk Receptor Tyrosine Kinases. Curr. Chem. Genomics, 2008, 1, 27-33.
- EJ Jung et al. Cytosolic accumulation of γH2AX is associated with tropomyosin-related kinase A-induced cell death in U2OS cells. Exp. Mol. Med. 2008, 40(3), 276–285.
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