GSK215
Based on 2 publication(s) in Google Scholar
GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect.
(Pink: FAK ligand (HY-13917); Blue: VHL ligand (HY-112078); Black: linker).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.26%
- No. CAS: 2743427-26-9
- Fòrmula: C50H59F3N10O6S
- Peso molecular:985.13
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) GSK215
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Actividad biológica
PROTAC; pDC50: 8.4 (FAK)[1]
GSK215 (0.1-1000 nM; 2 h) effectively increases the FAK degradation by >90% and determines a DC50 of 1.3 nM in A549 cells[1].
GSK215 induced degradation is proteasome and ubiquitin dependent[1].
GSK215 (above 100 nM, 6h) reduces primarily kinases CDK7, RPS6KA3, MET and GAK[1].
GSK215 (100 nM, 48 h) inhibits migration, invasion and collagen deposition in A549 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:0.1-1000 nM
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Incubation Time:2 h
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Result:Increased the FAK degradation.
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Cell Line:A549 cells
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Concentration:100 nM
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Incubation Time:48 h
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Result:Inhibited cell migration.
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Cell Line:A549 cells
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Concentration:100 nM
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Incubation Time:48 h
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Result:Inhibited cell invasion.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male CD1 mice (P878/881A), 7-9 weeks[1]
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Dosage:8 mg/kg
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Administration:Single subcutaneous injection
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Result:Caused a rapid and profound degradation of FAK in liver over time, with a maximal degradation of ~85% being achieved within 18 h. Endogenous FAK was found to still be reduced by ~60% at 96 h post-dose.The Cmax and tmax were 526 ng/mL and 0.33 hours, respectively.
Chemical Information
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No. CAS 2743427-26-9
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Appearance Solid
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Peso molecular 985.13
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Fòrmula C50H59F3N10O6S
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Color Off-white to light yellow
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SMILES
O=C([C@H]1N(C([C@@H](NC(CN2CCN(C3=CC=C(NC4=NC=C(C(F)(F)F)C(NC5=CC=CC=C5C(NC)=O)=C4)C(OC)=C3)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C
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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 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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Sci Adv
Inhibition of focal adhesion kinase impairs tumor formation and preserves hearing in a murine model of NF2-related schwannomatosis. [Abstract]2026 Jan 30;12(5):eady8382. PMID: 41616055 -
Cell Signal
The role of FAK signaling in early placental development and trophoblast lineage specification in human pregnancy. [Abstract]2025 Oct:134:111946. PMID: 40553964
Solvente y solubilidad
DMSO : 250 mg/mL (253.77 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, 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.
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: ≥ 2.08 mg/mL (2.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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 (278 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, 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0151 mL | 5.0755 mL | 10.1509 mL | 25.3774 mL |
| 5 mM | 0.2030 mL | 1.0151 mL | 2.0302 mL | 5.0755 mL | |
| 10 mM | 0.1015 mL | 0.5075 mL | 1.0151 mL | 2.5377 mL | |
| 15 mM | 0.0677 mL | 0.3384 mL | 0.6767 mL | 1.6918 mL | |
| 20 mM | 0.0508 mL | 0.2538 mL | 0.5075 mL | 1.2689 mL | |
| 25 mM | 0.0406 mL | 0.2030 mL | 0.4060 mL | 1.0151 mL | |
| 30 mM | 0.0338 mL | 0.1692 mL | 0.3384 mL | 0.8459 mL | |
| 40 mM | 0.0254 mL | 0.1269 mL | 0.2538 mL | 0.6344 mL | |
| 50 mM | 0.0203 mL | 0.1015 mL | 0.2030 mL | 0.5075 mL | |
| 60 mM | 0.0169 mL | 0.0846 mL | 0.1692 mL | 0.4230 mL | |
| 80 mM | 0.0127 mL | 0.0634 mL | 0.1269 mL | 0.3172 mL | |
| 100 mM | 0.0102 mL | 0.0508 mL | 0.1015 mL | 0.2538 mL |
GSK215 Related Classifications
HY-132296 Related Classifications
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