Vevorisertib trihydrochloride
Based on 2 publication(s) in Google Scholar
Vevorisertib trihydrochloride (ARQ 751 trihydrochloride) is an orally active allosteric AKT inhibitor that blocks AKT phosphorylation. Vevorisertib trihydrochloride inhibits tumor cell proliferation through Cyclin D1 and Ki67. Vevorisertib trihydrochloride inhibits liver fibrosis through collagen accumulation, alpha-SMA, COL1, and TGF-beta. Vevorisertib trihydrochloride reduces total bilirubin. Vevorisertib trihydrochloride significantly reduces tumor size in a cirrhotic rat HCC model. Vevorisertib trihydrochloride can be used for research on hepatocellular carcinoma.
For research use only. We do not sell to patients.
- Purity : 98.05%
- CAS No.: 1416775-08-0
- Formula: C35H41Cl3N8O
- Molecular Weight:696.11
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Vevorisertib trihydrochloride
More
Biological Activity
Description
IC50 & Target
[1]|
Akt1 0.55 nM (IC50) |
Akt2 0.81 nM (IC50) |
Akt3 1.31 nM (IC50) |
Akt1 1.2 nM (Kd) |
Akt1E17K 8.6 nM (Kd) |
In Vitro
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Fischer 344 (male, six-week-old, DEN-induced cirrhotic HCC model)[1]
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Dosage:10 mg/kg/day
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Administration:p.o.; daily (5 days on, 9 days off); 15 days over 6 weeks
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Result:Reduced mean tumor size to 4.3 mm compared to 9.9 mm in control.
Decreased number of tumors on the liver surface by 63% (36.6) compared to control (100.4).
Reduced frequencies of Cyclin D1-positive nuclei in the tumor area to 20.1 compared to 58.9 in control.
Decreased frequency of Ki67+ tumor cells to 9.3 compared to 43.7 in control.
Reduced liver fibrosis to 55.1% compared to 100% in control.
Downregulated expression of fibrosis marker α-SMA in liver tissue compared to control.
Lowered serum levels of total bilirubin compared to control.
- Western Blot
- Collagen: Sirius Red Staining
- BrdU Incorporation Assay
- Somatic Cell Culture
- Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Liver Cancer Modeling
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- Liver Histomorphometry
- Kinase activity and phosphorylation assays
- Fibrosis/Collagen Morphometry
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Protocol for Kinase activity and phosphorylation assays
- MTT Cell Proliferation Assay
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1416775-08-0
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Appearance Solid
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Molecular Weight 696.11
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Formula C35H41Cl3N8O
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Color White to yellow
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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
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Synonyms
ARQ 751 trihydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Death Discov
NRG1/PDGFC loop between fibroblasts and cancer cells drives paclitaxel resistance via ferroptosis suppression in breast cancer. [Abstract]2025 Nov 10;11(1):520. PMID: 41213930 -
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (143.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 25 mg/mL (35.91 mM; ultrasonic and warming and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5.25 mg/mL (7.54 mM); Clear solution
This protocol yields a clear solution of ≥ 5.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (52.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5.25 mg/mL (7.54 mM); Clear solution
This protocol yields a clear solution of ≥ 5.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (52.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (290 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.4366 mL | 7.1828 mL | 14.3655 mL | 35.9139 mL |
| 5 mM | 0.2873 mL | 1.4366 mL | 2.8731 mL | 7.1828 mL | |
| 10 mM | 0.1437 mL | 0.7183 mL | 1.4366 mL | 3.5914 mL | |
| 15 mM | 0.0958 mL | 0.4789 mL | 0.9577 mL | 2.3943 mL | |
| 20 mM | 0.0718 mL | 0.3591 mL | 0.7183 mL | 1.7957 mL | |
| 25 mM | 0.0575 mL | 0.2873 mL | 0.5746 mL | 1.4366 mL | |
| 30 mM | 0.0479 mL | 0.2394 mL | 0.4789 mL | 1.1971 mL | |
| DMSO | 40 mM | 0.0359 mL | 0.1796 mL | 0.3591 mL | 0.8978 mL |
| 50 mM | 0.0287 mL | 0.1437 mL | 0.2873 mL | 0.7183 mL | |
| 60 mM | 0.0239 mL | 0.1197 mL | 0.2394 mL | 0.5986 mL | |
| 80 mM | 0.0180 mL | 0.0898 mL | 0.1796 mL | 0.4489 mL | |
| 100 mM | 0.0144 mL | 0.0718 mL | 0.1437 mL | 0.3591 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Vevorisertib trihydrochloride Related Classifications
HY-137458A Related Classifications
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