AC-4-130-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAC-4-130Cat.No.:HY-124500CASNo.:1834571-82-2分?式:C??H??ClF?N?O?S分?量:751.2作?靶點:STAT作?通路:JAK/STATSignaling;StemCell/Wnt儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:100mg/mL(133.12mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.3312mL6.6560mL13.3120mL5mM0.2662mL1.3312mL2.6624mL10mM0.1331mL0.6656mL1.3312mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.33mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性AC-4-130?種有效的STAT5SH2結構域抑制劑。AC-4-130直接與STAT5結合并破壞STAT5激活、?聚化、核易位和STAT5依賴性因轉錄。AC-4-130在FLT3-ITD驅動的??病細胞中誘導細胞周期停滯和細胞凋亡。AC-4-130具有抗癌活性，可以有效阻斷急性髓系??病(AML)中STAT5活性的病理?平。IC50&TargetSTAT5體外研究AC-4-130(0.1-100μM;72hours)leadstoasignificantincreaseinapoptosisinadose-dependentandtime-dependentmannerinMV4-11orMOLM-13cells[1].AC-4-130(2,5μM;72hours)inducescellcyclearrestwithanincreaseinG0/G1arrestedcellsandaconcomitantreductionincellsinSorG2/M[1].AC-4-130(0.5-2;24hours)revealsreducedpY-STAT5levelsbothinthecytoplasmandnucleus[1].AC-4-130-mediatedSTAT5inhibitionefficientlyblockstheproliferationandclonogenicgrowthofprimaryhumanAMLcells,whilehealthyCD34+cellsarelesssensitive[1].REFERENCES[1].BettinaWingelhofer,etal.PharmacologicinhibitionofSTAT5inacutemyeloidleukemia.Leukemia.2018May;32(5):1135-1146.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-82