Vevorisertib (ARQ 751) trihydrochloride 是选择性、变构、pan-AKT 和 AKT1-E17K 突变抑制剂，可有效抑制 AKT 的磷酸化。Vevorisertib trihydrochloride 对 AKT1 和 AKT1-E17K 的 Kd 值分别为 1.2 nM 和 8.6 nM。Vevorisertib trihydrochloride 对 AKT1、AKT2 和 AKT3 的 IC₅₀ 值分别为 0.55、0.81 和 1.3 nM。 Vevorisertib trihydrochloride 可用于癌症的研究。

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.

Solid

Akt1 0.55 nM (IC50) Akt2 0.81 nM (IC5

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 (GI50 < 1 μM).
Vevorisertib trihydrochloride exhibits strong anti-proliferative activity in PIK3CA muta

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Yu Y, et al. Targeting AKT1-E17K and the PI3K/AKT Pathway with an Allosteric AKT Inhibitor, ARQ 092. PLoS One. 2015 Oct 15;10(10):e0140479.
[2]. Kozinova M, et al. Combined Inhibition of AKT and KIT Restores Expression of Programmed Cell Death 4 (PDCD4) in Gastrointestinal Stromal Tumor. Cancers (Basel). 2021 Jul 23;13(15):3699.

In Vitro: DMSO : 150 mg/mL (215.48 mM; Need ultrasonic)H₂O : 25 mg/mL (35.91 mM; ultrasonic and warming and heat to 60°C)配制储备液