PF-04217903 phenolsulfonate
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 100mg | $650 | Check With Us |
| 250mg | $1250 | Check With Us |
| 500mg | $1875 | Check With Us |
: Cat #: V39597 CAS #: 1159490-85-3 Purity ≥ 99%
Description: PF-04217903 phenolsulfonate is a novel, highly potent and ATP-competitive inhibitor of c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met and has antiangiogenic properties.
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| Molecular Weight (MW) | 546.56 |
|---|---|
| Molecular Formula | C25H22N8O5S |
| CAS No. | 1159490-85-3 |
| SMILES Code | O=S(C1=CC=C(O)C=C1)(O)=O.OCCN2N=CC(C3=CN=C4C(N(CC5=CC=C6N=CC=CC6=C5)N=N4)=N3)=C2 |
| Synonyms | PF-04217903 phenolsulfonate; PF04217903 phenolsulfonate; PF 04217903 phenolsulfonate |
| Protocol | In Vitro | PF-04217903 phenolsulfonate 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 phenolsulfonate (1.5-3333 nM; 48 hours) induces apoptosis of GTL-16 cells (IC50=31 nM). PF-04217903 phenolsulfonate (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. |
|---|---|---|
| In Vivo | PF-04217903 phenolsulfonate (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 phenolsulfonate strongly induces phospho-PDGFRβ levels in U87MG xenograft tumors. PF-04217903 phenolsulfonate (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.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.8296 mL | 9.1481 mL | 18.2963 mL | 36.5925 mL |
| 5mM | 0.3659 mL | 1.8296 mL | 3.6593 mL | 7.3185 mL |
| 10mM | 0.1830 mL | 0.9148 mL | 1.8296 mL | 3.6593 mL |
| 20mM | 0.0915 mL | 0.4574 mL | 0.9148 mL | 1.8296 mL |
The molarity calculator equation
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
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%ddH2O
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Method for preparing DMSO master liquid:
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,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.