ProductDescription
PF-2341066(Crizotinib)isanorally-available,ATP-competitive,aminopyridine-baseddualinhibitorofc-MetandALKwithIC50of11nMand24nM,respectively.[1]AkinaseselectivitypanelshowsthatPF-2341066isselectiveagainstmosttyrosineandserine-threoninekinases,withmodestactivitywithRon(IC50,80nM).[2]PF-2341066inhibitsc-Metphosphorylationandc-Met-dependentproliferation,migration,andinvasionofhumantumorcellsinvitroatIC50sof5to20nM.
PF-2341066hasbeenshowntobeeffectiveinosteosarcomagrowth[3]andanaplasticlarge-celllymphomas[4].
Technicalinformation:
| ChemicalFormula: | C21H22Cl2FN5O | |
| CAS#: | 877399-52-5 | |
| MolecularWeight: | 450.34 | |
| Purity: | >99% | |
| Appearance: | White | |
| ChemicalName: | 3-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine | |
| Solubility: | Upto40mMinDMSO | |
| Synonyms: | Crizotinib,PF-02341066,PF-2341066,PF2341066,PF2341066 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Zouetal.,Anorallyavailablesmall-moleculeinhibitorofc-Met,PF-2341066,exhibitscytoreductiveantitumorefficacythroughantiproliferativeandantiangiogenicmechanisms.CancerRes.2007,67,4408-4417.PubmedID:17483355 |
| 2. | Cuietal.,Structurebaseddrugdesignofcrizotinib(PF-02341066),apotentandselectivedualinhibitorofmesenchymal-epithelialtransitionfactor(c-MET)kinaseandanaplasticlymphomakinase(ALK).J.Med.Chem.2011,54,6342-6363.PubmedID:21812414 |
| 3. | Sampsonetal.,TheorallybioavailablemetinhibitorPF-2341066inhibitsosteosarcomagrowthandosteolysis/matrixproductioninaxenograftmodel.J.Bone.Miner.Res.2011,26(6),1283-1294.PubmedID:21308771 |
| 4. | Christensenetal.,CytoreductiveantitumoractivityofPF-2341066,anovelinhibitorofanaplasticlymphomakinaseandc-Met,inexperimentalmodelsofanaplasticlarge-celllymphoma.Mol.CancerTher.2007,6,3314-3322.PubmedID:21812414 |
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