PF 04217903 mesylate
Chemical Name: 4-[1-(6-Quinolinylmethyl)-1H-1,2,3-triazolo[4,5-b]pyrazin-6-yl]-1H-pyrazole-1-ethanol mesylate
Purity: ≥98%
Biological Activity
PF 04217903 mesylate is a highly selective, high affinity MET inhibitor (Ki = 6-7 nM against wild type c-Met). Displays >1000-fold selectivity for c-Met over a panel of 208 kinases.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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Acquired resistance to anti-EGFR mAb ICR62 in cancer cells is accompanied by an increased EGFR expression, HER-2/HER-3 signalling and sensitivity to pan HER blockers.
Khelwatty S, Essapen S, Seddon A, Fan Z, Modjtahedi H
Br J Cancer, 2015;113(7):1010-9. -
Novel therapeutic inhibitors of the c-Met signaling pathway in cancer.
Eder et al.
Clin.Cancer Res., 2009;15:2207 -
Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors.
Timofeevski et al.
Biochemistry, 2009;48:5339 -
Discovery of small molecule c-Met inhibitors: evolution and profiles of clinical candidates.
Underiner et al.
Anticancer Agents Med.Chem., 2010;10:7 -
Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-
Cui et al.
J.Med.Chem., 2012;55:8091
Product Datasheets
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Citations for PF 04217903 mesylate
The citations listed below are publications that use Tocris products. Selected citations for PF 04217903 mesylate include:
3 Citations: Showing 1 - 3
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Blood vessel endothelium-directed tumor cell streaming in breast tumors requires the HGF/C-Met signaling pathway.
Authors: Leung Et al.
Oncogene 2017;36:2680
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CD44 plays a functional role in Helicobacter pylori-induced epithelial cell proliferation.
Authors: Bertaux-Skeirik Et al.
PLoS Pathog 2015;11:e1004663
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Tuftsin signals through its receptor neuropilin-1 via the transforming growth factor beta pathway.
Authors: Stella E Et al.
J Neurochem 2013;127:394-402
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