ProductDescription
SU-6668(TSU-68)isanATP-competitive,oxindole-basedinhibitorofFlk-1/KDR,PDGFRb,andFGFR1phosphorylationwithKivaluesof2.1,0.008,and1.2uM,respectively.[1]Attheseinhibitorylevels,itwasshownthatSU-6668inducesantiangiogenicandproapoptoticeffectsinvivo.[2,3].OraladmiNISTrationofSU6668inducedtumorregressioninA431,PC-3,NCI-HT29,andColo205celllines,andtumorstasisinSF767TgliomaandNCI-H460celllines.[2]
Inhumanmyeloidleukemiacelllinesandacutemyeloidleukemiablasts,SU6668wasshowntoinhibitthestemcellfactor-inducedphosphorylationofc-kitandERK1/2andinducedapoptosis.[4]
Technicalinformation:
ChemicalFormula: | C18H18N2O3 | |
CAS#: | 252916-29-3 | |
MolecularWeight: | 310.35 | |
Purity: | >98% | |
Appearance: | Orange | |
ChemicalName: | (Z)-3-(2,4-dimethyl-5-((2-oxoindolin-3-ylidene)methyl)-1H-pyrrol-3-yl)propanoicacid | |
Solubility: | Upto100mMinDMSO | |
Synonyms: | SU6668,SU-6668,Orantinib,TSU68 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
1. | Lairdetal.,SU6668isapotentantiangiogenicandantitumoragentthatinducesregressionofestablishedtumors.CancerRes.2000,60,4152-4160.PubmedID:10945623 |
2. | Lairdetal.,SU6668inhibitsFlk-1/KDRandPDGFRbetainvivo,resultinginrapidapoptosisoftumorvasculatureandtumorregressioninmice.FASEB,2002,16(7),681-690.PubmedID:11978732 |
3. | Marzolaetal.,InvivoassessmentofantiangiogenicactivityofSU6668inanexperimentalcoloncarcinomamodel.Clin.CancerRes.2004,10,739-750.PubmedID:14760097 |
4. | Smolichetal.,TheantiangiogenicproteinkinaseinhibitorsSU5416andSU6668inhibittheSCFreceptor(c-kit)inahumanmyeloidleukemiacelllineandinacutemyeloidleukemiablasts.Blood,2001,97,1413-1421.PubmedID:11978732 |
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