Bozitinib-PLB-1001-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBozitinibCat.No.:HY-125017CASNo.:1440964-89-5Synonyms:PLB-1001;CBT-101;Vebreltinib分?式:C??H??F?N?分?量:424.38作?靶點(diǎn):c-Met/HGFR作?通路:ProteinTyrosineKinase/RTK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:50mg/mL(117.82mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.3564mL11.7819mL23.5638mL5mM0.4713mL2.3564mL4.7128mL10mM0.2356mL1.1782mL2.3564mL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:≥2.08mg/mL(4.90mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.90mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.90mM);ClearsolutionBIOLOGICALACTIVITY?物活性Bozitinib(PLB-1001)?種可通過?腦屏障的?選擇性c-MET激酶抑制劑。Bozitinib(PLB-1001)ATP競爭性?分?抑制劑，與酪氨酸激酶超家族的常規(guī)ATP結(jié)合?袋結(jié)合。體外研究Bozitinib(PLB-1001)(30μM;6hours)inhibitsthephosphorylationofMETandSTAT3,hasarobustinhibitoryeffectofPLB-1001onMETanditsdownstreamsignalingpathways.WesternBlotAnalysis[1]CellLine:Humanastrocytes(HA)cellsConcentration:30μMIncubationTime:6hoursResult:Decreasedp-STAT3,p-METexpression.REFERENCES[1].HuH,etal.MutationalLandscapeofSecondaryGlioblastomaGuidesMET-TargetedTrialinBrainTumor.Cell.2018Nov29;175(6):1665-1678.e18.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3