产品展示更多>>
- ABT-199 1257044-40-8

- ABT-199 1257044-40-8
ABT-199 1257044-40-8
产品描述 描述 ABT-199 is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Phase 3.
纯度 >98%储存/保存方法 Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.基本信息 别名 维奈妥拉;Venetoclax;GDC-0199外观 Yellow solid可溶性/溶解性 DMSO : 77.5 mg/mL (89.24 mM; Need ultrasonic)生物活性 靶点 Bcl-2 FamilyIn vitro(体外研究) ABT-199 shows less sensitivity to Bcl-xL, Mcl-1 and Bcl-w with Ki of 48 nM, > 444 nM and 245 nM, respectively. ABT-199 potently inhibits FL5.12-Bcl-2 cells, RS4;11 cells with EC50 of 4 nM and 8 nM, while shows low activity against FL5.12-Bcl-xL cells with EC50 of 261 nM. ABT-199 induces a rapid apoptosis in RS4;11 cells with cytochrome c release, caspase activation, the externalization of phosphatidylserine and the accumulation of sub-G0/G1 DNA. Quantitative immunoblotting reveals that sensitivity to ABT-199 correlated strongly with the expression of Bcl-2, including NHL, DLBCL, MCL, AML and ALL cell lines. ABT-199 also induces apoptosis in CLL with an average EC50 of 3.0 nM.In vivo(体内研究) ABT-199 (100 mg/kg) causes a maximal tumor growth inhibition of 95% and tumor growth delay of 152% in RS4;11 xenografts. ABT-199 also inhibits xenograft growth (DoHH2, Granta-519) as a single agent or in combination with SDX-105 and other agents.研究领域 研究领域 CancerCancer MetabolismCellular metabolic processCancerCancer MetabolismResponse to hypoxiaCancerCell DeathApoptosisMetabolismCancerCell DeathApoptosisApoptosis MarkersBcl 2 familyCancerInvasion/microenvironmentApoptosisBcl 2 familyCancerOncoproteins/suppressorsOncoproteinsCell survival & deathCancerTumor biomarkersOncoproteinsApoptosisIntracellularBcl2 FamilyMetabolismTypes of diseaseCancerMetabolismPathways and ProcessesMetabolism processesApoptosisMetabolismPathways and ProcessesMetabolism processesHypoxiaMetabolismPathways and ProcessesMitochondrial MetabolismMitochondrial markersSignal TransductionMetabolismMitochondrialDrug DiscoverySmall Molecule DrugLead Compound DiscoveryABT-199 1257044-40-8温馨提示:本产品仅作科研实验使用,不支持临床等研究
