1. Protein Tyrosine Kinase/RTK
  2. c-Met/HGFR
  3. PF-04217903

PF-04217903 

Cat. No.: HY-12017 Purity: 99.64%
Handling Instructions

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

For research use only. We do not sell to patients.

PF-04217903 Chemical Structure

PF-04217903 Chemical Structure

CAS No. : 956905-27-4

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10 mM * 1  mL in DMSO USD 92 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of PF-04217903:

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Description

PF-04217903 is a potent ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met. PF-04217903 shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties[1][2].

IC50 & Target

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

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].

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].

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.
Clinical Trial
Molecular Weight

372.38

Formula

C₁₉H₁₆N₈O

CAS No.

956905-27-4

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (53.71 mM; Need ultrasonic)

Ethanol : < 1 mg/mL (insoluble)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.64%

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Keywords:

PF-04217903PF04217903PF 04217903c-Met/HGFRGTL-16gastriccarcinomamigrationlungcolonphosphorylationphospho-PDGFRβInhibitorinhibitorinhibit

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Product name:
PF-04217903
Cat. No.:
HY-12017
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