Cat. No.: HY-12017

PF-04217903

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

PF-04217903 is a potent ATP-competitive c-Met kinase inhibitor with K_i of 4.8 nM for human c-Met. PF-04217903 shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties.

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Pureté: 99.85%
CAS No.: 956905-27-4
Formule: C₁₉H₁₆N₈O
Masse moléculaire:372.38

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PF-04217903 Chemical Structure

CAS No.: 956905-27-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

Ki: 4.8 nM (human c-Met)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>10000 nM Compound: Chemical Probe: PF-04217903	Antiproliferative activity against human A549 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay Antiproliferative activity against human A549 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay	[PMID: 22389468]
A549	IC₅₀	0.004 μM Compound: 2, PF-04217903	Antagonist activity at c-MET receptor in human A549 cells assessed as inhibition of autophosphorylation after 1 hr by ELISA Antagonist activity at c-MET receptor in human A549 cells assessed as inhibition of autophosphorylation after 1 hr by ELISA	[PMID: 22924734]
COLO 205	IC₅₀	>10000 nM Compound: Chemical Probe: PF-04217903	Antiproliferative activity against human COLO 205 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay Antiproliferative activity against human COLO 205 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay	[PMID: 22389468]
DLD-1	IC₅₀	>10000 nM Compound: Chemical Probe: PF-04217903	Antiproliferative activity against human DLD-1 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay Antiproliferative activity against human DLD-1 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay	[PMID: 22389468]
HCC1143	IC₅₀	>10000 nM Compound: Chemical Probe: PF-04217903	Antiproliferative activity against human HCC1143 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay Antiproliferative activity against human HCC1143 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay	[PMID: 22389468]
HCT-116	IC₅₀	>10000 nM Compound: Chemical Probe: PF-04217903	Antiproliferative activity against human HCT-116 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay	[PMID: 22389468]
HT-29	IC₅₀	>10000 nM Compound: Chemical Probe: PF-04217903	Antiproliferative activity against human HT-29 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay	[PMID: 22389468]
HT-29	IC₅₀	7 nM Compound: Chemical Probe: PF-04217903	Inhibition of cell invasion in HGF-stimulated human HT-29 cells over expressing c-Met incubated for 48 hrs by Matrigel based analysis Inhibition of cell invasion in HGF-stimulated human HT-29 cells over expressing c-Met incubated for 48 hrs by Matrigel based analysis	[PMID: 22389468]
HUVEC	IC₅₀	12.3 nM Compound: Chemical Probe: PF-04217903	Antiproliferative activity against HGF-stimulated HUVEC cells assessed as reduction in cell viability after 48 to 72 hrs by MTT assay Antiproliferative activity against HGF-stimulated HUVEC cells assessed as reduction in cell viability after 48 to 72 hrs by MTT assay	[PMID: 22389468]
HUVEC	IC₅₀	27 nM Compound: Chemical Probe: PF-04217903	Inhibition of cell invasion in HGF-stimulated HUVEC cells incubated for 48 hrs by Matrigel based analysis Inhibition of cell invasion in HGF-stimulated HUVEC cells incubated for 48 hrs by Matrigel based analysis	[PMID: 22389468]
HUVEC	IC₅₀	7.3 nM Compound: Chemical Probe: PF-04217903	Induction of apoptosis in HGF-stimulated HUVEC cells assessed as increase in apoptotic cells incubated for 48 hrs by ELISA Induction of apoptosis in HGF-stimulated HUVEC cells assessed as increase in apoptotic cells incubated for 48 hrs by ELISA	[PMID: 22389468]
MDA-MB-231	IC₅₀	>10000 nM Compound: Chemical Probe: PF-04217903	Antiproliferative activity against human MDA-MB-231 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay	[PMID: 22389468]
MDA-MB-468	IC₅₀	>10000 nM Compound: Chemical Probe: PF-04217903	Antiproliferative activity against human MDA-MB-468 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay	[PMID: 22389468]
NCI-H1993	IC₅₀	30 nM Compound: Chemical Probe: PF-04217903	Antiproliferative activity against human NCI-H1993 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay Antiproliferative activity against human NCI-H1993 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay	[PMID: 22389468]
NCI-H1993	IC₅₀	33.6 nM Compound: PF-4217903	Cytotoxicity against human NCI-H1993 cells assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against human NCI-H1993 cells assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 27448775]
NCI-H441	IC₅₀	11 nM Compound: Chemical Probe: PF-04217903	Inhibition of cell migration in HGF-stimulated human NCI-H441 cells over expressing c-Met incubated for 48 hrs by Matrigel based analysis Inhibition of cell migration in HGF-stimulated human NCI-H441 cells over expressing c-Met incubated for 48 hrs by Matrigel based analysis	[PMID: 22389468]
NCI-H441	IC₅₀	12.5 nM Compound: Chemical Probe: PF-04217903	Inhibition of cell invasion in HGF-stimulated human NCI-H441 cells over expressing c-Met incubated for 48 hrs by Matrigel based analysis Inhibition of cell invasion in HGF-stimulated human NCI-H441 cells over expressing c-Met incubated for 48 hrs by Matrigel based analysis	[PMID: 22389468]
PC-3	IC₅₀	>10000 nM Compound: Chemical Probe: PF-04217903	Antiproliferative activity against human PC-3 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay	[PMID: 22389468]
SW-620	IC₅₀	>10000 nM Compound: Chemical Probe: PF-04217903	Antiproliferative activity against human SW620 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay Antiproliferative activity against human SW620 cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay	[PMID: 22389468]
U-87MG ATCC	IC₅₀	>10000 nM Compound: Chemical Probe: PF-04217903	Antiproliferative activity against human U-87 MG cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay Antiproliferative activity against human U-87 MG cells over expressing c-Met assessed as reduction in cell viability after 48 to 72 hrs by MTT assay	[PMID: 22389468]

In Vitro

PF-04217903 (0.1-10000 nM; 48-72 hours) inhibits proliferation of c-Met–amplified human GTL-16 gastric carcinoma and H1993 NSCLC cells with IC₅₀ values of 12 and 30 nM, respectively^[1].
PF-04217903 (1.5-3333 nM; 48 hours) induces apoptosis of GTL-16 cells (IC₅₀=31 nM)^[1].
PF-04217903 also inhibits HGF-mediated cell migration and Matrigel invasion in several c-Met–overexpressing tumor cell lines such as human NCI-H441 lung carcinoma and HT29 colon carcinoma with IC₅₀ values comparable with those for inhibition of c-Met phosphorylation in these cell lines (IC₅₀=7-12.5 nM)^[1]. PF-04217903 displays similar potency to inhibit the activity of c-Met-H1094R, c-Met-R988C, and c-Met-T1010I with IC₅₀ of 3.1 nM, 6.4 nM, and 6.7 nM, respectively, but has no inhibitory activity against c-Met-Y1230C with IC₅₀ of >10 μM^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

GTL-16, H1993 cells
Concentration:

0.1, 1, 10, 100, 1000, 10000 nM
Incubation Time:

48-72 hours
Result:

Inhibited proliferation of c-Met–amplified human GTL-16 gastric carcinoma and H1993 NSCLC cells with IC₅₀ values of 12 and 30 nM, respectively.

Apoptosis Analysis^[1]

Cell Line:

GTL-16 cells
Concentration:

1.5-3333 nM
Incubation Time:

48 hours
Result:

Induced apoptosis of GTL-16 cells (IC₅₀=31 nM).

In Vivo

PF-04217903 (1-30 mg/kg; p.o.; daily for 16 days) shows dose-dependent tumor growth inhibition, which correlated with the inhibition in c-Met phosphorylation in these tumors^[1].
PF-04217903 (5-50 mg/kg, p.o.; once daily for 3 days) dose dependently inhibits c-Met, Gab-1, Erk1/2, and AKT phosphorylation and induced apoptosis (cleaved caspase-3) in U87MG xenograft tumors at all dose levels. PF-04217903 phenolsulfonate shows a significant dose-dependent reduction of human IL-8 levels in both the U87MG and GTL-16 models and decreases human VEGFA levels in the GTL-16 model. PF-04217903 strongly induces phospho-PDGFRβ levels in U87MG xenograft tumors^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female nu/nu mice (GTL-16 xenograft model)^[1]
Dosage:

1, 3, 10, 30 mg/kg
Administration:

Oral; daily for 16 days
Result:

Showed dose-dependent tumor growth inhibition, and was correlated with the inhibition in c-Met phosphorylation in these tumors.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 956905-27-4
Appearance Solid
Masse moléculaire 372.38
Formule C₁₉H₁₆N₈O
Color White to off-white
SMILES

OCCN1N=CC(C2=NC3=C(N=C2)N=NN3CC4=CC5=CC=CN=C5C=C4)=C1
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
JCI Insight

Injury-induced FoxM1 expression in mouse kidney drives epithelial proliferation by a Cyclin F dependent mechanism. [Abstract]

2024 Jun 25:e175416. PMID: 38916959

Solvant et solubilité

In Vitro:

DMSO : 20 mg/mL (53.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : < 1 mg/mL (insoluble)

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Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6854 mL

13.4271 mL

26.8543 mL

5 mM

0.5371 mL

2.6854 mL

5.3709 mL

10 mM

0.2685 mL

1.3427 mL

2.6854 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2 mg/mL (5.37 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2 mg/mL (5.37 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2 mg/mL (5.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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Références

[1]. Zou HY, et al. Sensitivity of selected human tumor models to PF-04217903, a novel selective c-Met kinase inhibitor. Mol Cancer Ther. 2012 Apr;11(4):1036-47. [Content Brief]

[2]. Cui JJ, et al. 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-yl) [Content Brief]

[3]. Timofeevski SL, et al. Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors. Biochemistry, 2009, 48(23), 5339-5349. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6854 mL	13.4271 mL	26.8543 mL	67.1357 mL
	5 mM	0.5371 mL	2.6854 mL	5.3709 mL	13.4271 mL
	10 mM	0.2685 mL	1.3427 mL	2.6854 mL	6.7136 mL
	15 mM	0.1790 mL	0.8951 mL	1.7903 mL	4.4757 mL
	20 mM	0.1343 mL	0.6714 mL	1.3427 mL	3.3568 mL
	25 mM	0.1074 mL	0.5371 mL	1.0742 mL	2.6854 mL
	30 mM	0.0895 mL	0.4476 mL	0.8951 mL	2.2379 mL
	40 mM	0.0671 mL	0.3357 mL	0.6714 mL	1.6784 mL
	50 mM	0.0537 mL	0.2685 mL	0.5371 mL	1.3427 mL

Keywords

PF-04217903

2 Cited Publications

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PF-04217903

Kinase Inhibitor Library

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Publications Citing Use of MedChemExpress (MCE) PF-04217903

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

PF-04217903

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) PF-04217903

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

PF-04217903 Related Classifications

HY-12017 Related Classifications