Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBafetinibCat.No.:HY-50868CASNo.:859212-16-1Synonyms:INNO-406;NS-187分?式:C??H??F?N?O分?量:576.62作?靶點(diǎn):Bcr-Abl;Src;Apoptosis作?通路:ProteinTyrosineKinase/RTK;Apoptosis儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(173.42mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.7342mL8.6712mL17.3424mL5mM0.3468mL1.7342mL3.4685mL10mM0.1734mL0.8671mL1.7342mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(4.34mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.34mM);ClearsolutionBIOLOGICALACTIVITY?物活性Bafetinib具有抗腫瘤活性的，有效的，具有?服活性的Lyn/Bcr-Abl酪氨酸激酶抑制劑。Bafetinib通過Bcl-2家族調(diào)節(jié)的內(nèi)在凋亡途徑增強(qiáng)?種促凋亡的Bcl-2同性(BH)3-純蛋?(Bim、Bad、Bmf和Bik)的活性，并誘導(dǎo)Ph+??病細(xì)胞凋亡。戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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