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PF 04217903 mesylate
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.
Sold for research purposes under agreement from Pfizer Inc.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 468.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.13 mL||10.67 mL||21.35 mL|
|5 mM||0.43 mL||2.13 mL||4.27 mL|
|10 mM||0.21 mL||1.07 mL||2.13 mL|
|50 mM||0.04 mL||0.21 mL||0.43 mL|
References are publications that support the biological activity of the product.
Eder et al (2009) Novel therapeutic inhibitors of the c-Met signaling pathway in cancer. Clin.Cancer Res. 15 2207 PMID: 19318488
Timofeevski et al (2009) Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors. Biochemistry 48 5339 PMID: 19459657
Underiner et al (2010) Discovery of small molecule c-Met inhibitors: evolution and profiles of clinical candidates. Anticancer Agents Med.Chem. 10 7 PMID: 20015007
Cui et al (2012) 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- J.Med.Chem. 55 8091 PMID: 22924734
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2 Citations for PF 04217903 mesylate
Citations are publications that use Tocris products. Selected citations for PF 04217903 mesylate include:
Bertaux-Skeirik et al (2015) CD44 plays a functional role in Helicobacter pylori-induced epithelial cell proliferation. PLoS Pathog 11 e1004663 PMID: 25658601
Leung et al (2017) Blood vessel endothelium-directed tumor cell streaming in breast tumors requires the HGF/C-Met signaling pathway. Oncogene 36 2680 PMID: 27893712
Do you know of a great paper that uses PF 04217903 mesylate from Tocris? Please let us know.
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