• Obatoclax,alsoknownasGX15-070,isanovelBcl-2homologydomain-3(BH3)mimetic.ItoccupiesahydrophobiccleftwithintheBH3bindinggrooveofBcl-2,antagonizingBcl-2andthusinducingapoptosis.Chonghaile,T.N.andLetai,A."MimickingtheBH3domaintokillcancercells."Oncogene27:S149-S157(2008).
• Obatoclaxinhibitedprimaryacutemyeloidleukemia(AML)ProgenitorcellproliferationwithanaverageIC50of0.18±0.07µM.ObatoclaxpotentlyinducedapoptosisinprimaryAMLcellswithanaverageIC50of3.6±1.2µM.Konopleva,M.,etal."MechanismsofantileukemicactivityofthenovelBcl-2homologydomain-3mimeticGX15-070(Obatoclax)."CancerRes.68:3413-3420(2008).
• ObatoclaxhadasynergisticantitumoreffectwiththenovelBH3mimeticABT-737oninducingapoptosisinOCI-AML3cells.ItalsohadasynergisticantitumoreffectwithAraC(1-β-D-arABInofuranosylcytosine)oninducingapoptosisinleukemiccelllinesandprimaryAMLsamples.Konopleva,M.,etal."MechanismsofantileukemicactivityofthenovelBcl-2homologydomain-3mimeticGX15-070(Obatoclax)."CancerRes.68:3413-3420(2008).
• ObatoclaxovercomesBcl-2-,Bcl-xL-,Bcl-w-,andMcl-1-mediatedresistancetoBAXorBAK.ObatoclaxalsoovercomestheMcl-1-conferedresistancetotheBCL-2/BCL-XL/BCL-w-selectiveantagoNISTABT-737andtotheproteasomeinhibitorbortezomib.Nguyen,M.,etal."Smallmoleculeobatoclax(GX15-070)antagonizesMCL-1andovercomesMCL-1-mediatedresistancetoapoptosis."Proc.Natl.Acad.Sci.USA104:19512-19517(2007).
• ObatoclaxreleasedBakfromMcl-1andBcl-xLandinducedapoptosisinmantlecelllymphoma(MCL)celllinesandprimarycellsfrompatientswithMCL.Obatoclaxneutralizedbortezomib-inducedMcl-1accumulationandcooperatedwithNoxatoinduceBakdisplacementfromthisprotein,andsynergizedwithbortezomibandsensitizedMCLcellstolowdosesofthisproteasomeinhibitor.Pérez-Galán,P.,etal."TheBH3-mimeticGX15-070synergizeswithbortezomibinmantlecelllymphomabyenhancingNoxa-mediatedactivationofBak."Blood109:4441-4449(2007).
• Obatoclaxaugmentedtumornecrosisfactor-relatedapoptosis-inducingligand(TRAIL)-mediatedapoptosis,possIBLybyreleasingBakandBimfromBcl-2/Bcl-xLorMcl-1proteinsinhumanpancreaticcancercells.Huang,S.,etal."BH3mimeticobatoclaxenhancesTRAIL-mediatedapoptosisinhumanpancreaticcancercells."Clin.CancerRes.15:150-159(2009).
• ObatoclaxinhibitedinfluenzaAvirus(IAV)uptakeanddemonstratedbroad-spectrumantiviralactivity.Denisova,O.V.,etal."Obatoclax,saliphenylhalamide,andgemcitabineinhibitinfluenzaAvirusinfection."J.Biol.Chem.287:35324-35332(2012).
• RelatedCASnumber:803712-67-6forthefreebase.
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• ThisproductisofferedforR&Duseinaccordancewith(i)35USC271(e)+A13(1)intheU.S.;(ii)Section69.1ofJapanesePatentLawinJapan;(iii)Section11,No.2oftheGermanPatentActof1981inGermany;(iv)Section60,Paragraph5boftheU.K.PatentsActof1977intheU.K.;(v)Sections55.2(1)and55.2(6)andothercommonlawexemptionsofCanADIanpatentlaw;(vi)Section68BofthePatentsActof1953inNewZealandtogetherwiththeamendmentofsamebytheStatutesAmendmentBillof2002;(vii)suchrelatedlegislationand/orcaselawasmaybeorbecomeapplicableintheaforementionedcountries;and(viii)suchsimilarlawsandrulesasmayapplyinvariousothercountries.
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