上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
Vevorisertib (Synonyms: ARQ 751)
Vevorisertib (ARQ 751) 是一种具有口服活性、有效和选择性的 pan-AKT 丝氨酸/苏氨酸激酶抑制剂,对 AKT1 (IC50=0.55 nM)、AKT2 (IC50=0.81 nM) 和AKT3 (IC50=1.31 nM) 有抑制作用。Vevorisertib 单体化合物或与其他抗癌化合物联用,可用于 PIK3CA/AKT/PTEN 突变的实体瘤研究。
Vevorisertib Chemical Structure
CAS No. : 1416775-46-6
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Vevorisertib 的其他形式现货产品:
生物活性 |
Vevorisertib (ARQ 751) is an orally active, potent and selective pan-AKT serine/threonine kinase inhibitor against AKT1 (IC50=0.55 nM), AKT2 (IC50=0.81 nM), and AKT3 (IC50=1.31 nM). Vevorisertib, as a single agent or in combination with other anti-cancer agents, can be used for the research of solid tumors with PIK3CA / AKT / PTEN mutations[1][2][3][4]. |
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IC50 & Target[4] |
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体外研究 (In Vitro) |
Vevorisertib binds to wild-type AKT1 and mutant AKT1-E17K with Kd of 1.2 nM and 8.6 nM, respectively, and suppresses pAKT(S473) in 293T cells transiently transfected with AKT1-E17K[4]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
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]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
586.73 |
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Formula |
C35H38N8O |
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CAS 号 |
1416775-46-6 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
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参考文献 |
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