Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETL02-59Cat.No.:HY-112852CASNo.:1315330-17-6分?式:C??H??F?N?O?分?量:609.64作?靶點(diǎn):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:125mg/mL(205.04mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.6403mL8.2016mL16.4031mL5mM0.3281mL1.6403mL3.2806mL10mM0.1640mL0.8202mL1.6403mL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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)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%salineSolubility:≥2.08mg/mL(3.41mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.41mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.41mM);ClearsolutionBIOLOGICALACTIVITY?物活性TL02-59?種具有?服活性，選擇性的Src-家族激酶Fgr抑制劑，IC50為0.03nM。TL02-59抑制Src-家族激酶Lyn和Hck，IC50分別為0.1nM和160nM。TL02-59有效抑制急性髓性??病(AML)細(xì)胞?長(zhǎng)。IC50&TargetIC50:0.03nM(Fgr),0.1nM(Lyn)and160nM(Hck)[1]體外研究TL02-59(0.1-1000nM;6hours)potentlyinhibitsFgrautophosphorylationinTF-1cells,withparitialinhibitionat0.1-1nMandcompleteinhibitionabove10nM.Hck,LynandFlt3areinhibitedinthe100to1000nMrange[1].TL02-59inhibitsthegrowthandinducedapoptosisofAMLcelllinesexpressingthiskinasewithsingle-digitnMpotency[1].TL02-59inducesgrowtharrestinprimaryAMLbonemarrowsamples[1].WesternBlotAnalysis[1]CellLine:TF-1myeloidcellsConcentration:0.1,1,10,100,1000nMIncubationTime:6hoursResult:InhibitedFgrautophosphorylationinTF-1cells.體內(nèi)研究TL02-59(oraladministration;1and10mg/kg;forthreeweeks)completelyeliminatesAMLcellsfromthespleenandperipheralbloodinamousemodelofAML,whiledramaticallysuppressingbonemarrowinvolvement[1].TL02-59hasat1/2of5.7hbyi.vinjectionand6.5hbyp.o.administration,respectively[1].AnimalModel:NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ(NSG)micewithhumanMV4-11AMLcells[1]Dosage:1and10mg/kgAdministration:Oral;forthreeweeksResult:EliminatedAMLcellsfromthespleenandperipheralbloodinamousemodelofAML,whiledramaticallysuppressingbonemarrowinvolvement.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?CellDeathDiscov.2021Nov12;7(1):349.?InVivo.Nov-Dec2021;35(6):3053-3066.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].WeirMC,etal.SelectiveInhibitionoftheMyeloidSrc-FamilyKinaseFgrPotentlySuppressesAMLCellGrowthinVitroandinVivo.ACSChemBiol.2018Jun15;13(6):1551-1559.McePdfHeightCaution:Producthasnotbeenfullyvalidatedf