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)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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.
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
Certificate of Analysis / Product Datasheet
Safety Datasheet
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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
Keywords: PF 04217903 mesylate, supplier, pfizer, PF04217903, c-met, met, mesenchymal, epithelial, transition, factor, hgfr, receptors, tyrosine, kinase, rtk, inhibitors, inhibits, anticancer, selective, MET, Receptors, MET, Receptors, Tocris Bioscience
Tocris Bioscience是一家专卖生命科学研究chemicals, peptides and antibodies的知名品牌,其产品也广为各大药厂、大学、研究机构,超过五万名科学研究者所采用。 目前,產品內容已超過一千六百種以上,並每年持續不斷的增加新的產品。目前,产品内容已超过一千六百种以上,并每年持续不断的增加新的产品。
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