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Submit ReviewPF 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.
Sold for research purposes under agreement from Pfizer Inc.
PF 04217903 mesylate is also offered as part of the Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
分子量 | 468.49 |
公式 | C19H16N8O.CH3SO3H |
储存 | Store at +4°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 46.85 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: 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
引用文献是使用了 Tocris 产品的出版物。 PF 04217903 mesylate 的部分引用包括:
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
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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