PROTAC FAK degrader 1
Based on 8 publication(s) in Google Scholar
PROTAC FAK degrader 1 (Compound PROTAC-3) is a selective and effective degrader of Fak PROTAC with a DC50 of 3.0 nM. PROTAC FAK degrader 1 reduces the ability of cancer cells to migrate and invade. PROTAC FAK degrader 1 can be used in the study of tumor.
(Pink: FAK ligand (HY-44146); Blue: VHL ligand (HY-125845); Black: linker (HY-44141)).
For research use only. We do not sell to patients.
- Purity: 99.25%
- CAS No.: 2301916-69-6
- Formula: C47H56F3N9O8S2
- Molecular Weight:996.13
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Storage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PROTAC FAK degrader 1
More- Nucleic Acids Res. 2023 Oct 13;51(18):e93. [Abstract]
- Sci Adv. 2026 Jan 30;12(5):eady8382. [Abstract]
- Structure. 2024 Dec 5;32(12):2352-2363.e8. [Abstract]
- Cancer Res Commun. 2024 Dec 1;4(12):3165-3179. [Abstract]
- Exp Cell Res. 2021 Nov 15;408(2):112868. [Abstract]
- Front Oncol. 2022 Apr 28;12:851065. [Abstract]
- Patent. US20250041303A1.
- bioRxiv. 2023 Jan 24.
All PROTACs Isoforms
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Biological Activity
IC50: 6.5 nM (Focal adhesion kinase)
DC50: 3.0 nM (Focal adhesion kinase) in PC3 cells[1]
PROTAC FAK degrader 1 (0.5 nM-10 μM; 24 h) induces high-efficiency Fak degradation in PC3 cells in a dose-dependent manner, and significantly inhibits the phosphorylation levels of paxillin and Akt downstream of Fak[1].
PROTAC FAK degrader 1 (50-250 nM; 24 h) reduces the migration and invasion ability of MDA-MB-231 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC3 cells
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Concentration:0.5, 1, 5, 10, 50, 100 nM and 1 μM
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Incubation Time:24 h
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Result:Reduced the level of Fak in a dose-dependent manner.
Chemical Information
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CAS No. 2301916-69-6
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Appearance Solid
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Molecular Weight 996.13
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Formula C47H56F3N9O8S2
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Color White to off-white
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SMILES
O=C(N[C@H](C(N1[C@H](C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)C[C@@H](O)C1)=O)C(C)(C)C)CCOCCOC4=CC=C(NC5=NC(NCC6=CC=CC(N(C)S(C)(=O)=O)=C6)=C(C(F)(F)F)C=N5)C=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (8)
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Journal Impact Factor
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Most Recent
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Nucleic Acids Res
Recovery of protein synthesis to assay DNA repair activity in transcribed genes in living cells and tissues. [Abstract]2023 Oct 13;51(18):e93. PMID: 37522336 -
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 -
Structure
PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062 -
Cancer Res Commun
2024 Dec 1;4(12):3165-3179. PMID: 39585085 -
Exp Cell Res
FAK-targeting PROTAC demonstrates enhanced antitumor activity against KRAS mutant non-small cell lung cancer. [Abstract]2021 Nov 15;408(2):112868. PMID: 34648846 -
Front Oncol
FAK PROTAC Inhibits Ovarian Tumor Growth and Metastasis by Disrupting Kinase Dependent and Independent Pathways. [Abstract]2022 Apr 28;12:851065. PMID: 35574330 -
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Solvent & Solubility
DMSO : 200 mg/mL (200.78 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 (stored under nitrogen). 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 (stored under nitrogen). 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: ≥ 5 mg/mL (5.02 mM); Suspended solution
This protocol yields a suspended solution of ≥ 5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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.
Purity & Documentation
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Data Sheet (274 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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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 (stored under nitrogen). 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 | 1.0039 mL | 5.0194 mL | 10.0389 mL | 25.0971 mL |
| 5 mM | 0.2008 mL | 1.0039 mL | 2.0078 mL | 5.0194 mL | |
| 10 mM | 0.1004 mL | 0.5019 mL | 1.0039 mL | 2.5097 mL | |
| 15 mM | 0.0669 mL | 0.3346 mL | 0.6693 mL | 1.6731 mL | |
| 20 mM | 0.0502 mL | 0.2510 mL | 0.5019 mL | 1.2549 mL | |
| 25 mM | 0.0402 mL | 0.2008 mL | 0.4016 mL | 1.0039 mL | |
| 30 mM | 0.0335 mL | 0.1673 mL | 0.3346 mL | 0.8366 mL | |
| 40 mM | 0.0251 mL | 0.1255 mL | 0.2510 mL | 0.6274 mL | |
| 50 mM | 0.0201 mL | 0.1004 mL | 0.2008 mL | 0.5019 mL | |
| 60 mM | 0.0167 mL | 0.0837 mL | 0.1673 mL | 0.4183 mL | |
| 80 mM | 0.0125 mL | 0.0627 mL | 0.1255 mL | 0.3137 mL | |
| 100 mM | 0.0100 mL | 0.0502 mL | 0.1004 mL | 0.2510 mL |
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