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Vevorisertib(ARQ 751,维沃色替)是一种口服活性、强效和选择性泛-AKT丝氨酸/苏氨酸激酶抑制剂,对AKT1/AKT2/AKT3均有抑制作用,常用于研究具有PIK3CA/AKT/PTEN突变的实体瘤,显示出剂量依赖性的抗肿瘤活性。
Vevorisertib(ARQ 751,维沃色替)是一种口服活性、强效和选择性泛-AKT丝氨酸/苏氨酸激酶抑制剂,对AKT1/AKT2/AKT3均有抑制作用,常用于研究具有PIK3CA/AKT/PTEN突变的实体瘤,显示出剂量依赖性的抗肿瘤活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 567 | 现货 | |
5 mg | ¥ 1,130 | 现货 | |
10 mg | ¥ 1,590 | 现货 | |
25 mg | ¥ 2,870 | 现货 | |
50 mg | ¥ 3,930 | 现货 |
产品描述 | Vevorisertib (ARQ 751) is an orally active, potent and selective pan-AKT serine/threonine kinase inhibitor with inhibitory effects on AKT1/AKT2/AKT3 and is commonly used in the study of solid tumors with PIK3CA/AKT/PTEN mutations, showing dose-dependent antitumor activity. |
靶点活性 | Akt1:0.55 nM, Akt1:0.55 nM (IC50), Akt2:0.81 nM, Akt3:1.31 nM, Akt3:1.31 nM (IC50), Akt2:0.81 nM (IC50) |
体外活性 | Vevorisertib binds to wild-type AKT1 and mutant AKT1-E17K with K d of 1.2 nM and 8.6 nM, respectively, and suppresses pAKT(S473) in 293T cells transiently transfected with AKT1-E17K[4]. |
体内活性 | Vevorisertib (10~120 mg/kg) exerts dose-dependent anti-tumor activity in an AKT1-E17K mutant endometrial patient-derived xenograft (PDX) model. Vevorisertib shows a plasma half-life of 4 to 5 hours and no tissue accumulation[4]. |
别名 | 维沃色替, ARQ751, ARQ 751 |
分子量 | 586.73 |
分子式 | C35H38N8O |
CAS No. | 1416775-46-6 |
Smiles | O=C(N(C)C1CCN(C2=CC=CC(=C2)C3=NC4=C(N=C(C5=CC=CN=C5N)N4C6=CC=C(C=C6)C7(N)CCC7)C=C3)CC1)C |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||
溶解度信息 | DMSO: 4.00 mg/mL (6.82 mM), Sonication is recommended. | |||||||||||||||
溶液配制表 | ||||||||||||||||
DMSO
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