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Merck
CN

SML0263

PF-04217903

≥98% (HPLC)

别名:

4-[1-(6-Quinolinylmethyl)-1H-1,2,3-triazolo[4,5-b]pyrazin-6-yl]-1H-pyrazole-1-ethanol methanesulfonate (1:1)

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关于此项目

经验公式(希尔记法):
C19H16N8O·CH3SO3H
化学文摘社编号:
分子量:
468.49
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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产品名称

PF-04217903, ≥98% (HPLC)

InChI

1S/C19H16N8O.CH4O3S/c28-7-6-26-12-15(9-22-26)17-10-21-18-19(23-17)27(25-24-18)11-13-3-4-16-14(8-13)2-1-5-20-16;1-5(2,3)4/h1-5,8-10,12,28H,6-7,11H2;1H3,(H,2,3,4)

SMILES string

CS(O)(=O)=O.OCCn1cc(cn1)-c2cnc3nnn(Cc4ccc5ncccc5c4)c3n2

InChI key

HBEMHKVWZJTVOC-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: ≥5 mg/mL (warmed)

storage temp.

2-8°C

Quality Level

Gene Information

human ... MET(4233)

Biochem/physiol Actions

PF-04217903 is a c-Met inhibitor.
PF-04217903 is a highly selective, potent inhibitor of the hepatocyte growth factor receptor c-Met. PF-04217903 inhibits endogenous, wild type c-Met in A549 human lung carcinoma cells with an IC50 of 4.8 nM. The compund displays 1000-fold selectivity against a panel of 208 other kinases.
PF-04217903 is an ATP-competitive inhibitor. It elicits antiangiogenic functionality. PF-04217903 inhibits c-Met phosphorylation in xenograft models leading to partial tumor growth suppression.

Application

PF-04217903 has been used as tyrosine-protein kinase Met (C-Met) selective inhibitor in Madin-Darby Canine kidney (MDCK) cells and NT2D1 non-seminoma cells.

Features and Benefits

This compound is featured on the Met page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number

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Sensitivity of selected human tumor models to PF-04217903, a novel selective c-Met kinase inhibitor
Zou HY, et al.
Molecular Cancer Therapeutics, 11(4), 1036-1047 (2012)
c-Src Recruitment is Involved in c-MET-Mediated Malignant Behaviour of NT2D1 Non-Seminoma Cells
Leonetti E, et al.
International Journal of Molecular Sciences, 20(2), 320-320 (2019)
c-MET receptor as potential biomarker and target molecule for malignant testicular germ cell tumors
Scheri K, et al.
Testing, 9(61), 31842-31842 (2018)
Erica Leonetti et al.
International journal of molecular sciences, 20(2) (2019-01-17)
: c-MET pathway over-activation is the signature of malignancy acquisition or chemotherapy resistance of many cancers. We recently demonstrated that type II Testicular Germ Cell Tumours (TGCTs) express c-MET receptor. In particular, we elucidated that the non-seminoma lesions express c-MET

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