PHA 665752
Tocris Bioscience, part of Bio-Techne | Catalog # 2693
Potent and selective MET inhibitor
Product Description
PHA 665752 is a potent, selective and ATP-competitive inhibitor of MET kinase (IC50 values are 9, 68, 200, 1400, 3000, 3800 and 6000 nM for MET, Ron, Flk-1, c-abl, FGFR1, EGFR and c-src respectively and > 10000 nM for IGF-IR, PDGFR, AURORA2, PKA, PKBα, p38α, MK2 and MK3). Antitumor agent; inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts.Licensing Information
Sold for research purposes under agreement from Pfizer Inc.Product Specifications
Molecular Weight
641.61
Formula
C32H34Cl2N4O4S
Storage
Store at +4°C
Purity
≥98% (HPLC)
Chemical Name
(2R)-1-[[5-[(Z)-[5-[[(2,6-Dichlorophenyl)methyl]sulfonyl]-1,2-dihydro-2-oxo-3H-indol-3-ylidene]methyl]-2,4-dimethyl-1H-pyrrol-3-yl]carbonyl]-2-(1-pyrrolidinylmethyl)pyrrolidine
CAS Number
477575-56-7
PubChem ID
10461815
InChI Key
OYONTEXKYJZFHA-SSHUPFPWSA-N
SMILES
ClC1=C(CS(C2=CC(/C(C(N4)=O)=C/C3=C(C)C(C(N5CCC[C@@H]5CN6CCCC6)=O)=C(C)N3)=C4C=C2)(=O)=O)C(Cl)=CC=C1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 64.16 | 100 |
Preparing Stock Solutions
for PHA 665752
The following data is based on the product molecular weight 641.61
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.56 mL | 7.79 mL | 15.59 mL |
| 5 mM | 0.31 mL | 1.56 mL | 3.12 mL |
| 10 mM | 0.16 mL | 0.78 mL | 1.56 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.31 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Smolen Amplification of MET may identify a subset of cancers with extreme sensitivity to the selective tyrosine kinase inhibitor PHA-665752. Proc.Natl.Acad.Sci.USA
- Puri A selective small molecule inhibitor of c-Met, PHA665752, inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts. Cancer Res. 2007 PMID: 17440059
- Tu Efficacy of c-Met inhibitor for advanced prostate cancer. BMC Cancer 2010 PMID: 20946682
- Christensen A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumour activity in vivo. Cancer Res. 2003 PMID: 14612533
Product Specific Notices for PHA 665752
For research use only
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