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PF 04217903 mesylate

Cat. No. 4239 3 Citations Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
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 (3)
Reviews
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for PF 04217903 mesylate

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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Compound Libraries for PF 04217903 mesylate

PF 04217903 mesylate is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for PF 04217903 mesylate

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 for PF 04217903 mesylate

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

Preparing Stock Solutions for PF 04217903 mesylate

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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets for PF 04217903 mesylate

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References for PF 04217903 mesylate

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

If you know of a relevant reference for PF 04217903 mesylate, please let us know.

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3 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

Stella E et al (2013) Tuftsin signals through its receptor neuropilin-1 via the transforming growth factor beta pathway. J Neurochem 127 394-402 PMID: 24033337

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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