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A-1155463是一种高效选择性的BCL-XL 抑制剂,对 BCL-XL 具有皮摩尔的结合亲和力,在Molt-4细胞中的EC50值为70 nM。
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A-1155463是一种高效选择性的BCL-XL 抑制剂,对 BCL-XL 具有皮摩尔的结合亲和力,在Molt-4细胞中的EC50值为70 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 472 | 现货 | |
5 mg | ¥ 970 | 现货 | |
10 mg | ¥ 1,380 | 现货 | |
25 mg | ¥ 2,480 | 现货 | |
50 mg | ¥ 3,720 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,460 | 现货 |
产品描述 | A-1155463, a highly potent and selective BCL-XL inhibitor, shows picomolar binding affinity to BCL-XL, and >1000-fold weaker binding to BCL-2 and related proteins BCL-W(Ki=19 nM) and MCL-1(Ki>440 nM). |
靶点活性 | BCL-XL:<0.01 nM(Ki) |
体外活性 | A-1155463在细胞中破坏BCL-XL-BIM复合体,但不影响BCL-2-BIM复合体。对于依赖BCL-XL的Molt-4细胞,A-1155463具有杀伤作用(EC50=70 nM),而对于依赖BCL-2的RS4;11细胞,则没有明显的细胞毒性(EC50>5 mM)。A-1155463能诱导凋亡的典型特征,包括线粒体释放细胞色素c、激活caspase以及BCL-XL依赖的H146细胞中caspase依赖的sub-G0-G1 DNA含量的积累。 |
体内活性 | 在非肿瘤SCID-Beige小鼠体内,单次以5 mg/kg IP方式给予A-1155463后,观察到血小板数量在给药后6小时内急剧下降,而后在72小时内恢复至正常水平。连续每日以5 mg/kg IP剂量对已接种BCL-XL依赖型H146肿瘤细胞的SCID-Beige小鼠进行14天治疗,显示出肿瘤生长受到统计学上显著的抑制(最大肿瘤生长抑制率=44%),该抑制效果在停药后消失[1]。 |
激酶实验 | Recombinant p38 isoforms are activated by Mkk6(E) under the following conditions: p38 (100 ng/mL), Mkk6(E) (30 ng/mL), ATP (100 mM) are mixed in kinase buffer (25 mM Hepes, 25 mM b-glycerophosphate, 0.1 mM sodium orthovanadate, 25 mM MgCl2, 2.5 mM DTT, pH 7.4) and incubated for 30 min at 30°C. A typical assay reaction for Mnk1 activity contained Mnk1 (2 ng/mL), HA-eIF4E (10 ng/mL), ATP (300 mM) in kinase buffer. The reaction is started by addition of activated p38 (0.03-3 ng/mL) and stopped after 30 min at 30°C by addition of SDS loading buffer. Inhibitors of Mnk1 are identified under the same assay conditions, except that Mnk1 is pre-activated using active p38a before exposure to the substrate and inhibitors. |
细胞实验 | Cells are treated with increasing concentration of A-1155463. Cells are assayed for viability after 72 h using the CellTiter-Glo luminescent cell viability assay according to the manufacturer's protocol. Results are normalized to cells without treatment. EC50 is calculated using the GraphPad Prism software.(Only for Reference) |
动物实验 | Animal Models: SCID-Beige MiceFormulation: 5% DMSO, 10% EtOH, 20% Cremaphor ELP, and 65% D5WDosages: 5 mg/kgAdministration: i.p. |
别名 | 醋酸艾塞那肽, A1155463, A 1155463 |
分子量 | 669.79 |
分子式 | C35H32FN5O4S2 |
CAS No. | 1235034-55-5 |
Smiles | C(NC1=NC=2C(S1)=CC=CC2)(=O)C3=C4C(CCN(C4)C5=NC(C(O)=O)=C(CCCOC6=C(F)C=C(C#CCN(C)C)C=C6)S5)=CC=C3 |
密度 | 1.45 g/cm3 (Predicted) |
存储 | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 100 mg/mL (149.3 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 100 mg/mL (149.3 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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