PF 04217903 mesylate

Name: PF 04217903 mesylate
Brand: Tocris Bioscience
SKU: 4239

Tocris Bioscience, part of Bio-Techne | Catalog # 4239

Citations (7)

COA / SDS

Highly selective MET inhibitor

Key Product Details

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)
Molecular Weight:	468.49

View Full Technical Details for PF 04217903 mesylate

Technical Data
Citations

Biological Activity for PF 04217903 mesylate

PF 04217903 mesylate is a highly selective, high affinity MET inhibitor (K_i = 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 for PF 04217903 mesylate

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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.

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 for PF 04217903 mesylate

References are publications that support the biological activity of the product.

Cui 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. 2012 PMID: 22924734
Timofeevski Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors. Biochemistry 2009 PMID: 19459657
Underiner Discovery of small molecule c-Met inhibitors: evolution and profiles of clinical candidates. Anticancer Agents Med.Chem. 2010 PMID: 20015007
Eder Novel therapeutic inhibitors of the c-Met signaling pathway in cancer. Clin.Cancer Res. 2009 PMID: 19318488