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Vevorisertib trihydrochloride

Catalog No. T38846 CAS 1416775-08-0

Synonyms: ARQ 751 trihydrochloride

Vevorisertib trihydrochloride (ARQ 751 trihydrochloride) is a selective and potent inhibitor of pan-AKT and AKT1-E17K mutations, inhibiting AKT1, AKT2 and AKT3. Vevorisertib trihydrochloride is used in the study of hepatocellular carcinoma and advanced solid tumours.

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Vevorisertib trihydrochloride Chemical Structure

Vevorisertib trihydrochloride, CAS 1416775-08-0

Pack Size	Availability	Price/USD
5 mg	In stock	$ 163.00
10 mg	In stock	$ 242.00
25 mg	In stock	$ 413.00
50 mg	In stock	$ 582.00
100 mg	In stock	$ 779.00

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Purity: 98.28%

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Description	Vevorisertib trihydrochloride (ARQ 751 trihydrochloride) is a selective and potent inhibitor of pan-AKT and AKT1-E17K mutations, inhibiting AKT1, AKT2 and AKT3. Vevorisertib trihydrochloride is used in the study of hepatocellular carcinoma and advanced solid tumours.
Targets&IC50	Akt1 (E17K):8.6 nM (Kd), Akt1:1.2 nM (Kd), Akt1:0.55 nM, Akt3:1.31 nM, Akt2:0.81 nM
In vitro	Vevorisertib trihydrochloride at concentrations ranging from 0 to 1000 nM over 2 hours inhibits the phosphorylation of AKT1-E17K. In NIH 3T3 cells transfected with pcDNAAKT-WT-GFP or pcDNA-E17K-GFP and treated with 1 μM of the compound for the same duration, it prevents the plasma membrane translocation of both AKT-WT and AKT1-E17K, regardless of growth factor presence. Additionally, a 5 μM concentration results in 57% inhibition of full-length AKT1. The compound demonstrates a dose-dependent impact on mTORC1 and AKT substrates, such as PRAS40, GSK3β, FOXO, BAD, and AS160 across various cancer cell lines with distinct concentrations (0 to 1 μM, 2 hours). It also exhibits significant anti-proliferative effects on esophageal, breast, and head and neck cancer cells, with GI 50 values below 1 μM, and showcases potent efficacy in PIK3CA mutant cell lines. Moreover, a combination of Vevorisertib trihydrochloride (MK-4440) and imatinib mesylate leads to cell cycle arrest and increased cell death in gastrointestinal stromal tumor cells. Western Blot analyses reveal the compound's effectiveness in inhibiting phosphorylation of AKT1-E17K and dose-dependent effects on mTORC1 and AKT substrates across different cell lines, including those with PIK3CA mutations and various cancer-related mutations.
In vivo	Vevorisertib trihydrochloride administered orally at doses of 25, 50, and 75 mg/kg for five consecutive days followed by a four-day break over a 20-day period demonstrated significant tumor growth inhibition rates of 68%, 78%, and 98%, respectively, in endometrial PDX mouse xenograft models featuring the AKT1-E17K mutation. When administered daily at varying doses (5, 10, 20, 40, 80, and 120 mg/kg) for ten days in AN3CA mouse xenograft models, it showed tumor growth inhibition rates ranging from 29% to 92%. The compound achieved C max plasma concentrations of ≥2 μM and was generally well-tolerated at all administered doses up to 120 mg/kg. Additionally, a combination of Vevorisertib trihydrochloride (MK-4440) and IM exhibited superior efficacy in an IM-sensitive preclinical GIST model compared to either agent alone, highlighting its potential as a robust therapeutic candidate in specific cancer models.

Synonyms	ARQ 751 trihydrochloride
Molecular Weight	696.12
Formula	C35H41Cl3N8O
CAS No.	1416775-08-0

Storage

store at low temperature,keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 20 mg/mL (28.73 mM)

DMSO: 100 mg/mL (143.66 mM), Sonication is recommended.

References and Literature

1. 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. 2. Yu Y, et al. Targeting AKT1-E17K and the PI3K/AKT Pathway with an Allosteric AKT Inhibitor, ARQ 09PLoS One. 2015 Oct 15;10(10):e0140479.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library

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Keywords

Vevorisertib trihydrochloride 1416775-08-0 Cytoskeletal Signaling PI3K/Akt/mTOR signaling Akt ARQ-751 Trihydrochloride ARQ751 Trihydrochloride ARQ751 ARQ-751 ARQ 751 Vevorisertib ARQ 751 trihydrochloride inhibitor inhibit

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