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AZD5153 6-Hydroxy-2-naphthoic acid (AZD5153) 是 AZD5153的6-羟基-2-萘甲酸盐形式。AZD5153是一种有口服活性的选择性 BET/BRD4溴结构域抑制剂,对BRD4的IC50值为1.7nM。
AZD5153 6-Hydroxy-2-naphthoic acid (AZD5153) 是 AZD5153的6-羟基-2-萘甲酸盐形式。AZD5153是一种有口服活性的选择性 BET/BRD4溴结构域抑制剂,对BRD4的IC50值为1.7nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 421 | 现货 | |
5 mg | ¥ 926 | 现货 | |
10 mg | ¥ 1,610 | 现货 | |
25 mg | ¥ 2,770 | 现货 | |
50 mg | ¥ 4,130 | 现货 | |
100 mg | ¥ 5,880 | 现货 | |
500 mg | ¥ 11,800 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,430 | 现货 |
产品描述 | AZD5153 6-Hydroxy-2-naphthoic acid (AZD5153) is a potent triazolopyridazine-based Bromodomain (BRD4) and Extraterminal (BET) inhibitor used in cancer treatments. |
靶点活性 | FL-BRD4:5 nM |
体外活性 | AZD5153处理显著影响MYC、E2F和mTOR的转录程序。值得注意的是,mTOR途径的调节与细胞系对AZD5153的敏感性有关。AZD5153强效破坏U2OS细胞中的BRD4焦点,IC50值为1.7 nmol/L。AZD5153有效降低细胞系中MYC蛋白水平,与其对AZD5153的敏感性无关。AML、MM和DLBCL细胞系对AZD5153高度敏感。 |
体内活性 | AZD5153 在AML异种移植瘤和人类全血中调节MYC和HEXIM1。体内给药后,AZD5153在急性髓性白血病、多发性骨髓瘤和弥漫性大B细胞性淋巴瘤的多个异种移植模型中导致肿瘤停滞或退缩。AZD5153通过口服给予携带MV-4-11异种移植瘤的小鼠,在给药后2、4、8小时测量药效活性(瘤内c-Myc水平)。观察到,在化合物游离血浆浓度<0.2 μM时,c-Myc表达在给药后8小时内显著减少。AZD5153治疗后c-Myc表达的减少与其他已发布的BET抑制剂一致。 |
细胞实验 | Apoptosis was analyzed by flow cytometry using CellEvent Caspase 3/7 Green detection reagent. MV-4-11, MM.1S, and K562 cells were pretreated with AZD5153 or I-BET762 for 48 hours in culture media. Cells were collected and stained with 5 μmol/L final concentration of CellEvent for 30 minutes at 37°C. Flow cytometry was done on a BD Fortessa using the Blue laser and FITC filter set. (Only for Reference) |
别名 | AZD5153, AZD5153结晶体(API形式), AZD-5153 HNT salt |
分子量 | 667.75 |
分子式 | C25H33N7O3·C11H8O3 |
CAS No. | 1869912-40-2 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 26 mg/mL (38.9 mM) DMSO: 93 mg/mL (139.3 mM) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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