PF 04217903 mesylate

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Cat.No. 4239 - PF 04217903 mesylate | C19H16N8O.CH3SO3H | CAS No. 956906-93-7
Description: Highly selective MET inhibitor
Chemical Name: 4-[1-(6-Quinolinylmethyl)-1H-1,2,3-triazolo[4,5-b]pyrazin-6-yl]-1H-pyrazole-1-ethanol mesylate
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Reviews
Literature

Biological Activity

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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M. Wt 468.49
Formula C19H16N8O.CH3SO3H
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 956906-93-7
PubChem ID 24852079
InChI Key HBEMHKVWZJTVOC-UHFFFAOYSA-N
Smiles OCCN1N=CC(C2=CN=C3C(N(CC4=CC=C(N=CC=C5)C5=C4)N=N3)=N2)=C1.CS(=O)(O)=O

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 46.85 100

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

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References

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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View all MET Receptor Inhibitors

Keywords: PF 04217903 mesylate, PF 04217903 mesylate supplier, pfizer, PF04217903, c-met, met, mesenchymal, epithelial, transition, factor, hgfr, receptors, tyrosine, kinase, rtk, inhibitors, inhibits, anticancer, selective, MET, Receptors, 4239, Tocris Bioscience

2 Citations for PF 04217903 mesylate

Citations are publications that use Tocris products. Selected citations for PF 04217903 mesylate include:

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

Bertaux-Skeirik et al (2015) CD44 plays a functional role in Helicobacter pylori-induced epithelial cell proliferation. PLoS Pathog 11 e1004663 PMID: 25658601


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Literature in this Area

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