1402438-74-7
Chemical Structure
PF-06273340
- CAS No.: 1402438-74-7
- Formula:C23H22ClN7O3
- Molecular Weight:479.92
IUPAC Name: N-(5-(2-amino-7-(1-hydroxy-2-methylpropan-2-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonyl)pyridin-3-yl)-2-(5-chloropyridin-2-yl)acetamide
InChIKey: BPIWZDNVMQQBQX-UHFFFAOYSA-N
SMILES: O=C(NC1=CC(C(C2=CN(C(C)(C)CO)C3=NC(N)=NC=C32)=O)=CN=C1)CC4=NC=C(Cl)C=C4
Biological Activity: PF-06273340 is a peripherally restricted pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, and TrkC receptors. PF-06273340 binds in a DFG-out conformation, targeting less conserved kinase ligand binding domain regions outside the ATP binding pocket. PF-06273340 exhibits anti-hyperalgesic and analgesic effects. PF-06273340 can be used for the research of pain[1][2].
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PF-06273340 | 98.8% | PF-06273340 is a peripherally restricted pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, and TrkC receptors. PF-06273340 binds in a DFG-out conformation, targeting less conserved kinase ligand binding domain regions outside the ATP binding pocket. PF-06273340 exhibits anti-hyperalgesic and analgesic effects. PF-06273340 can be used for the research of pain. | ||||||||||||||||||||
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- [1]. Skerratt S E, et al. The discovery of a potent, selective, and peripherally restricted pan-Trk inhibitor (PF-06273340) for the treatment of pain[J]. 2016.
- [2]. Loudon P, et al. Demonstration of an anti-hyperalgesic effect of a novel pan-Trk inhibitor PF-06273340 in a battery of human evoked pain models. Br J Clin Pharmacol. 2018;84(2):301-309. [Content Brief]
Keywords
