Vevorisertib
Based on 2 publication(s) in Google Scholar
Vevorisertib (ARQ 751) is an orally active allosteric AKT inhibitor that blocks AKT phosphorylation. Vevorisertib inhibits tumor cell proliferation through Cyclin D1 and Ki67. Vevorisertib inhibits liver fibrosis through collagen accumulation, alpha-SMA, COL1, and TGF-beta. Vevorisertib reduces total bilirubin. Vevorisertib significantly reduces tumor size in a cirrhotic rat HCC model. Vevorisertib can be used for research on hepatocellular carcinoma.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.03%
- CAS. Nr.: 1416775-46-6
- Formel: C35H38N8O
- Molecular Weight:586.73
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Vevorisertib
More
Biologische Aktivität
Beschreibung
IC50 & Target
[4]|
Akt1 0.55 nM (IC50) |
Akt2 0.81 nM (IC50) |
Akt3 1.31 nM (IC50) |
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
Chemical Information
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CAS. Nr. 1416775-46-6
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Appearance Solid
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Molecular Weight 586.73
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Formel C35H38N8O
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Color Light yellow 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
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Synonyms
ARQ 751
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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 -
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 6.67 mg/mL (11.37 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 0.67 mg/mL (1.14 mM); Clear solution
This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 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: ≥ 0.67 mg/mL (1.14 mM); Clear solution
This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (287 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)
Verweise
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. 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 |
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| DMSO | 1 mM | 1.7044 mL | 8.5218 mL | 17.0436 mL | 42.6090 mL |
| 5 mM | 0.3409 mL | 1.7044 mL | 3.4087 mL | 8.5218 mL | |
| 10 mM | 0.1704 mL | 0.8522 mL | 1.7044 mL | 4.2609 mL |
Vevorisertib Related Classifications
HY-137458 Related Classifications
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