LCH-7749944
Based on 5 publication(s) in Google Scholar
LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM. LCH-7749944 effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.68%
- No. CAS: 796888-12-5
- Fòrmula: C20H22N4O2
- Peso molecular:350.41
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) LCH-7749944
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Actividad biológica
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PAK4 14.93 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | EC50 |
7.7 μM
Compound: 23
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Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by Cell Titer-Glo assay
Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by Cell Titer-Glo assay
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[PMID: 28080063] |
LCH-7749944 (GNF-PF-2356; 5-50 μM; 24 hours) inhibits the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration dependent manner[1].
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LCH-7749944 (5-20 μM; 12-48 hours) induces apoptosis of SGC7901 cells[1].
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LCH-7749944 (5-20 μM; 12-48 hours) prominently induces a dose-dependent increase in the percentage of cells in G1 phase and decrease in S phase[1].
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LCH-7749944 (5-30 μM; 24 hours) dramatically decreases levels of phosphoPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MKN-1, BGC823, SGC7901 and MGC803 human gastric cancer cells
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Concentration:5, 10, 15, 20, 25, 30, 35, 40, 45, 50 μM
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Incubation Time:24 hours
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Result:Inhibited the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration dependent manner.
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Cell Line:SGC7901 cells
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Concentration:5, 10, 20 μM
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Incubation Time:12, 24, 48 hours
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Result:Induced apoptosis of SGC7901 cells.
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Cell Line:SGC7901 cells
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Concentration:5, 10, 20 μM
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Incubation Time:12, 24, 48 hours
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Result:Prominently induced a dose-dependent increase in the percentage of cells in G1 phase and decrease in S phase.
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Cell Line:SGC7901 cells
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Concentration:5, 10, 20, 30 μM
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Incubation Time:24 hours
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Result:Dramatically decreased levels of phosphoPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent manner.
Chemical Information
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No. CAS 796888-12-5
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Appearance Solid
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Peso molecular 350.41
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Fòrmula C20H22N4O2
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Color White to off-white
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SMILES
COC1=CC(NC2=NC(NCC3OCCC3)=C4C=CC=CC4=N2)=CC=C1
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Synonyms
GNF-PF-2356
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Cell
SARS-CoV-2 replication in airway epithelia requires motile cilia and microvillar reprogramming. [Abstract]2023 Jan 5;186(1):112-130.e20. PMID: 36580912 -
Adv Sci (Weinh)
Functional Phosphoproteomics in Cancer Chemoresistance Using CRISPR-Mediated Base Editors. [Abstract]2022 Oct;9(30):e2200717. PMID: 36045417 -
Int J Mol Sci
2024 Sep 21;25(18):10138. PMID: 39337621 -
Adv Biol (Weinh)
PAK4 is Required for Meiotic Resumption, Spindle Assembly, and Cortical Migration in Mouse Oocytes During Meiotic Maturation. [Abstract]2025 Jan;9(1):e2400307. PMID: 39435597 -
bioRxiv
Network analysis of α-synuclein pathology progression reveals p21-activated kinases as regulators of vulnerability. [Abstract]2024 Oct 22:2024.10.22.619411. PMID: 39484617
Solvente y solubilidad
DMSO : 250 mg/mL (713.45 mM; Need ultrasonic; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.17 mg/mL (6.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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: ≥ 2.17 mg/mL (6.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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.
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.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8538 mL | 14.2690 mL | 28.5380 mL | 71.3450 mL |
| 5 mM | 0.5708 mL | 2.8538 mL | 5.7076 mL | 14.2690 mL | |
| 10 mM | 0.2854 mL | 1.4269 mL | 2.8538 mL | 7.1345 mL | |
| 15 mM | 0.1903 mL | 0.9513 mL | 1.9025 mL | 4.7563 mL | |
| 20 mM | 0.1427 mL | 0.7134 mL | 1.4269 mL | 3.5672 mL | |
| 25 mM | 0.1142 mL | 0.5708 mL | 1.1415 mL | 2.8538 mL | |
| 30 mM | 0.0951 mL | 0.4756 mL | 0.9513 mL | 2.3782 mL | |
| 40 mM | 0.0713 mL | 0.3567 mL | 0.7134 mL | 1.7836 mL | |
| 50 mM | 0.0571 mL | 0.2854 mL | 0.5708 mL | 1.4269 mL | |
| 60 mM | 0.0476 mL | 0.2378 mL | 0.4756 mL | 1.1891 mL | |
| 80 mM | 0.0357 mL | 0.1784 mL | 0.3567 mL | 0.8918 mL | |
| 100 mM | 0.0285 mL | 0.1427 mL | 0.2854 mL | 0.7134 mL |
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