Bafetinib-INNO-406-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBafetinibCat.No.:HY-50868CASNo.:859212-16-1Synonyms:INNO-406;NS-187分⼦式:C₃₀H₃₁F₃N₈O分⼦量:576.62作⽤靶点:Bcr-Abl;Src;Apoptosis作⽤通路:ProteinTyrosineKinase/RTK;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(173.42mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7342mL8.6712mL17.3424mL5mM0.3468mL1.7342mL3.4685mL10mM0.1734mL0.8671mL1.7342mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(4.34mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.34mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Bafetinib具有抗肿瘤活性的，有效的，具有⼝服活性的Lyn/Bcr-Abl酪氨酸激酶抑制剂。Bafetinib通过Bcl-2家族调节的内在凋亡途径增强⼏种促凋亡的Bcl-2同性(BH)3-纯蛋⽩(Bim、Bad、Bmf和Bik)的活性，并诱导Ph+⽩⾎病细胞凋亡。户使⽤本产品发表的科研⽂献•Science.2017Dec1;358(6367):eaan4368.•SciTranslMed.2018Jul18;10(450).pii:eaaq1093.•FoodChemToxicol.2020Jan;135:110924.•JCancer.2019Jan29;10(5):1197-1208.•TechnicalUniversityofMunich.24.01.2018.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].GraceMS,etal.ThetyrosinekinaseinhibitorbafetinibinhibitsPAR2-inducedactivationofTRPV4channelsinvitroandpaininvivo.BrJPharmacol.2014Aug;171(16):3881-3894.[2].KimuraS,etal.NS-187,apotentandselectivedualBcr-Abl/Lyntyrosinekinaseinhibitor,isanovelagentforimatinib-resistantleukemia.Blood.2005Dec1;106(12):3948-3954.[3].KamitsujiY,etal.TheBcr-AblkinaseinhibitorINNO-406inducesautophagyanddifferentmodesofcelldeathexecutioninBcr-Abl-positiveleukemias.CellDeathDiffer.2008,15(11),1712-2172.[4].YokotaA,etal.INNO-406,anovelBCR-ABL/Lyndualtyrosinekinaseinhibitor,suppressesthegrowthofPh+leukemiacellsinthecentralnervoussystem,andcyclosporineAaugmentsitsinvivoactivity.Blood.2007,109(1),306-314.[5].KurodaJ,etal.Apoptosis-baseddualmoleculartargetingbyINNO-406,asecond-generationBcr-Ablinhibitor,andABT-737,aninhibitorofantiapoptoticBcl-2proteins,againstBcr-Abl-positiveleukemia.CellDeathDiffer.2007;14(9):1667-1677.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicat