PF 04217903 mesylate

Pricing Availability Delivery Time Qty
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 (1)
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.

All Tocris products are intended for laboratory research use only.

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 solvent 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

Safety Datasheet

References

References are publications that support the products' biological activity.

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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1 Citation 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


Do you know of a great paper that uses PF 04217903 mesylate from Tocris? If so please let us know.

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases

Pathways for PF 04217903 mesylate

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