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SML0263

Sigma-Aldrich

PF-04217903

≥98% (HPLC)

Synonym(s):

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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About This Item

Empirical Formula (Hill Notation):
C19H16N8O·CH3SO3H
CAS Number:
956906-93-7
Molecular Weight:
468.49
MDL number:
MFCD17392584
UNSPSC Code:
12352200
PubChem Substance ID:
329825271
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: ≥5 mg/mL (warmed)

storage temp.

2-8°C

SMILES string

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

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)

InChI key

HBEMHKVWZJTVOC-UHFFFAOYSA-N

Gene Information

human ... MET(4233)

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.

Biochem/physiol Actions

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.

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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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)
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)
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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