计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
2-8°C储存,干燥。低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Vevorisertib (ARQ 751) trihydrochloride is a selective, allosteric, pan- AKT and AKT1-E17K mutant inhibitors. Vevorisertib trihydrochloride potently inhibit phosphorylation of AKT . Vevorisertib trihydrochloride has Kd values of 1.2 nM and 8.6 nM for AKT1 and AKT1-E17K, respectively. Vevorisertib trihydrochloride has IC 50 values of 0.55, 0.81, and 1.3 nM for AKT1 , AKT2 , and AKT3 , respectively. Vevorisertib trihydrochloride can be used for the research of cancer
In Vitro
Vevorisertib trihydrochloride (0, 12, 33, 111, 333, 1000 nM, 2 hours) inhibits phosphorylation of AKT1-E17K. Vevorisertib trihydrochloride (1 μM for 2 hours; NIH 3T3 cells are transfected with either pcDNAAKT-WT-GFP or pcDNA-E17K-GFP) inhibits plasma membrane translocation of AKT-WT and AKT1-E17K irrespective of the presence of growth factors. Vevorisertib trihydrochloride (5 μM) exhibites 57% inhibition of full-length AKT1. Vevorisertib trihydrochloride (0, 0.012, 0.037, 0.11, 0.33, 1 μM; 2 hours) shows a dose-dependent effect on mTORC1 and AKT direct substrates including PRAS40, GSK3β, FOXO, BAD, and AS160 in cancer cell lines. Vevorisertib trihydrochloride has anti-proliferative effect on esophageal, breast, and head and neck cancer cells (GI 50 < 1 μM). Vevorisertib trihydrochloride exhibits strong anti-proliferative activity in PIK3CA mutant cell lines. Vevorisertib trihydrochloride (MK-4440)/imatinib mesylate (IM) combination shows cell cycle arrest, and increases cell death of gastrointestinal stromal tumor (GIST) cells. Vevorisertib trihydrochloride exhibits strong anti-proliferative activity in PIK3CA mutant cell lines: Breast Cancer Cell Lines GI 50 (nM) PIK3CA ER PR HER2 T47D 1.05 H1047R + + - EFM-19 1.54 H1047R + + - MCF-7 2.20 E545K + + - BT474 3.25 K111N + + + MDA-MB-453 6.05 H1047R - - + MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: 293T cells (transiently transfected with pcDNA-E17K-GFP) Concentration: 0, 12, 33, 111, 333, 1000 nM Incubation Time: 2 hours Result: Inhibited phosphorylation of AKT1-E17K. Western Blot AnalysisCell Line: Cancer cell lines: MDA-MB 453 (PIK3CAH1047R; Her2 amp), NCI-H1650 (PTEN ), KU-19-19 (AKT1-E17K&E49K; NRas Q61R) Concentration: 0, 0.012, 0.037, 0.11, 0.33, 1 μM Incubation Time: 2 hours Result: Showed a dose-dependent effect on mTORC1 and AKT direct substrates including PRAS40, GSK3β, FOXO, BAD, and AS160.
In Vivo
Vevorisertib trihydrochloride (25, 50 and 75 mg/kg; p.o.; 5 days dosing followed by a 4 day dosing holiday for 20 days) shows potent tumor growth inhibition of 68, 78 and 98%, respectively . Vevorisertib trihydrochloride (5, 10, 20, 40, 80, and 120 mg/kg; p.o. daily for ten days) shows tumor growth inhibition of 29, 33, 50, 73, 83, and 92%, respectively . Vevorisertib trihydrochloride reachs C max plasma concentrations of ≥2 μM . Vevorisertib trihydrochloride is generally well-tolerated at dose levels up to 120 mg/kg . Vevorisertib trihydrochloride (MK-4440)/IM combination shows superior efficacy in an IM-sensitive preclinical model of GIST compared with either single agent. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Endometrial PDX mouse xenograft models (AKT1-E17K mutation tumor fragments subcutaneously implanted in athymic nude mice; tumor volume of approximately 200 mm 3 ) Dosage: 25, 50 and 75 mg/kg Administration: p.o.; 5 days dosing followed by a 4 day dosing holiday for 20 days Result: Showed potent tumor growth inhibition of 68, 78 and 98%, respectively. Animal Model: AN3CA mouse xenograft models (female NCr nu/nu mice with 250 mm 3 tumors size) Dosage: 5, 10, 20, 40, 80, and 120 mg/kg Administration: p.o.; daily for ten days Result: Showed tumor growth inhibition of 29, 33, 50, 73, 83, and 92%, respectively.
Form:Solid
IC50& Target:Akt1 0.55 nM (IC 50 ) Akt2 0.81 nM (IC 50 ) Akt3 1.31 nM (IC 50 ) Akt1 1.2 nM (Kd) Akt1 E17K 8.6 nM (Kd)
规格
别名
维沃瑞替布三盐酸盐
规格或纯度
≥99%
英文名称
Vevorisertib trihydrochloride
生化机理
Vevorisertib (ARQ 751) 三盐酸盐是一种选择性、异位、泛 AKT 和 AKT1-E17K 突变体抑制剂。Vevorisertib 三盐酸盐能有效抑制 AKT 的磷酸化。Vevorisertib trihydrochloride 对 AKT1 的 Kd 值分别为 1.2 nM 和 8.6 nM。
储存条件
2-8°C储存,干燥
运输条件
低温运输
纯度
≥99%
名称和识别符
分子类型
小分子
Smiles
NC1=C(C=CC=N1)C2=NC3=CC=C(C4=CC(N(CC5)CCC5N(C)C(C)=O)=CC=C4)N=C3N2C6=CC=C(C7(CCC7)N)C=C6.[H]Cl.[H]Cl.[H]Cl
分子量
696.11
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 150 mg/mL (215.48 mM; Need ultrasonic) H2O : 25 mg/mL (35.91 mM; ultrasonic and warming and heat to 60°C)
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
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