PF-04217903 mesylate

This product is for research use only, not for human use. We do not sell to patients.

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Size	Price	Stock
250mg	$810	Check With Us
500mg	$1350	Check With Us
1g	$2025	Check With Us

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Cat #: V4454 CAS #: 956906-93-7 (mesylate) Purity ≥ 98%

Description: PF-04217903 mesylate, the methanesulfonate salt of PF-04217903, is a novel, potent, orally bioavailabe, selective, and ATP-competitive small-molecule tyrosine kinase inhibitor of c-Met with IC50 of 4.8 nM in A549 cell line and with anticancer activity, it is susceptible to oncogenic mutations (with no activity to Y1230C mutant).

References: 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.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	468.49
Molecular Formula	C20H20N8O4S
CAS No.	956906-93-7 (mesylate)
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 50 mg/mLr
	Water: <1 mg/mLr
	Ethanol: <1 mg/mL
Solubility In Vivo	1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
SMILES Code	OCCN1N=CC(C2=CN=C3C(N(CC4=CC=C5N=CC=CC5=C4)N=N3)=N2)=C1.OS(=O)(C)=O
Synonyms	PF04217903 mesylate; PF 04217903; PF-04217903; PF4217903 mesylate; PF-4217903; PF 4217903 mesylate

Protocol	In Vitro	PF-04217903 mesylate 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). PF-04217903 mesylate induces apoptosis of GTL-16 cells (IC50=31 nM). PF-04217903 mesylate (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.
Protocol	In Vivo	PF-04217903 mesylate (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 mesylate 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 mesylate strongly induces phospho-PDGFRβ levels in U87MG xenograft tumors. PF-04217903 mesylate (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.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	2.1345 mL	10.6726 mL	21.3452 mL	42.6903 mL
5mM	0.4269 mL	2.1345 mL	4.2690 mL	8.5381 mL
10mM	0.2135 mL	1.0673 mL	2.1345 mL	4.2690 mL
20mM	0.1067 mL	0.5336 mL	1.0673 mL	2.1345 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

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

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.