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| 品牌 | absin | CAS | 1257044-40-8 |
|---|---|---|---|
| 分子式 | C45H50ClN7O7S | 纯度 | ＞98% |
| 分子量 | 868.44 | 货号 | abs810559 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | is a Bcl-2-selective inhibitor with Ki o | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
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 Family |
| In 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 process CancerCancer MetabolismResponse to hypoxia CancerCell DeathApoptosisMetabolism CancerCell DeathApoptosisApoptosis MarkersBcl 2 family CancerInvasion/microenvironmentApoptosisBcl 2 family CancerOncoproteins/suppressorsOncoproteinsCell survival & death CancerTumor biomarkersOncoproteins ApoptosisIntracellularBcl2 Family MetabolismTypes of diseaseCancer MetabolismPathways and ProcessesMetabolism processesApoptosis MetabolismPathways and ProcessesMetabolism processesHypoxia MetabolismPathways and ProcessesMitochondrial MetabolismMitochondrial markers Signal TransductionMetabolismMitochondrial Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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