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- A-1210477 1668553-26-1
- A-1210477 1668553-26-1
A-1210477 1668553-26-1
产品描述 描述 A-1210477 is a potent and selective MCL-1 and Bcl-2 inhibitor with Ki and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members.
纯度 99%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 可溶性/溶解性 10 mM in DMSO生物活性 靶点 MCL-1In vitro(体外研究) In H929 cells, A-1210477 binds to MCL-1 with high affinity and induces MCL-1 protein elevation. In H929, H2110, and H23 cells, A-1210477 induce the hallmarks of apoptosis, and inhibits MCL-1-dependent cell viability. A-1210477 also synergizes with navitoclax to kill a variety of cancer cell lines. In SKBR3 cells, A-1210477 inhibits MCL-1–BIM interaction and induces classical features of apoptosis. In addition, A-1210477 sensitizes non-Hodgkin's lymphoma cell lines to venetoclax (ABT-199).参考文献 参考文献 1. Bruncko M, et al. J Med Chem. 2015 Mar 12;58(5):2180-2194.
2. Leverson JD, et al. Cell Death Dis. 2015 Jan 15;6:e1590.
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 DiscoveryA-1210477 1668553-26-1温馨提示：本产品仅作科研实验使用，不支持临床等研究