Ifebemtinib
Based on 3 publication(s) in Google Scholar
Ifebemtinib (BI 853520) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1 nM). Ifebemtinib shows anti-proliferative activity against cancer cells. Ifebemtinib inhibits FER Kinase and FES Kinase with IC50s of 900 nM and 1040 nM, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.64%
- CAS. Nr.: 1227948-82-4
- Formel: C28H28F4N6O4
- Molecular Weight:588.55
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Speicherung:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Ifebemtinib
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Biologische Aktivität
IC50: 1 nM (recombinant FAK)[1], 900 nM (FER Kinase), 1040 nM (FES Kinase)[3]
Ifebemtinib (BI 853520) (0-3 μM; 2 h) inhibits cancer cells growth[2].
Ifebemtinib (BI 853520) (0-30 μM; 4-6 d) represses tumor cell proliferation and invasion only in 3D culture[1].
Ifebemtinib (0-10 μM; 24 h) represses Y397-FAK autophosphorylation[1].
Ifebemtinib (0.1 μM; 96 h) shows a fast and potent inhibition of FAK in this highly metastatic murine breast cancer cell line[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC-3 cells
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Concentration:0-3 μM
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Incubation Time:2 hours
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Result:Resulted in a concentration-dependent reduction of the signal with a median EC50 value of 1 nM.
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Cell Line:4T1, Py2T, and Py2T-LT cells
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Concentration:0-30 μM
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Incubation Time:4-6 days
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Result:Indicated that the specific inhibition of cell proliferation and invasion at low doses is functional only in three-dimensional cell culture conditions, whereas cells cultured on plastic only respond to BI 853520 at very high, toxic doses.
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Cell Line:4T1, Py2T, and Py2T-LT cells
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Concentration:0-10 μM
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Incubation Time:24 hours
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Result:Reduced Y397-FAK autophosphorylation in all cell types.
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Cell Line:4T1, Py2T, and Py2T-LT cells
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Concentration:0.1 μM
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Incubation Time:96 hours
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Result:Decreased Y397-FAK autophosphorylation following 0.1 µM BI 853520 treatment occurred within 10 min and was substantially reduced at least for the following 48 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:FVB/N, Balb/c, or immunodeficient nude (nu/nu) mice transplanted with Py2T, 4T1, or MTflECad cells, respectively[1]
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Dosage:50 mg/kg
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Administration:Oral gavage; 50 mg/kg; once daily; 0-8 weeks
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Result:Decreased tumor volume significantly over time.
Chemical Information
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CAS. Nr. 1227948-82-4
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Appearance Solid
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Molecular Weight 588.55
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Formel C28H28F4N6O4
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Color White to off-white
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SMILES
O=C(C1=C(F)C=C(NC2=NC=C(C(F)(F)F)C(OC3=CC=CC4=C3C(N(C4)C)=O)=N2)C(OC)=C1)NC5CCN(CC5)C
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Synonyms
BI-853520; IN-10018
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (3)
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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 -
Anticancer Drugs
Upregulation of CDC25B by transcription factor TEAD4 drives invasion and inhibits cisplatin sensitivity through cell adhesion in stomach adenocarcinoma. [Abstract]2024 Nov 1;35(10):922-931. PMID: 39079173 -
bioRxiv
Decreased substrate stiffness leads to mitochondrial dysfunctions and Endothelial to Mesenchymal transition through Focal Adhesion Kinase activity in corneal endothelial cells. [Abstract]2025 Dec 2:2025.11.08.687366. PMID: 41279848
Lösungsmittel & Löslichkeit
DMSO : 60 mg/mL (101.95 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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)
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: ≥ 2.5 mg/mL (4.25 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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 (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Hirt UA, et al. Efficacy of the highly selective focal adhesion kinase inhibitor BI 853520 in adenocarcinoma xenograft models is linked to a mesenchymal tumor phenotype. Oncogenesis. 2018 Feb 23;7(2):21. [Content Brief]
[2]. Stefanie Tiede, et al. The FAK inhibitor BI 853520 exerts anti-tumor effects in breast cancer. Oncogenesis. 2018 Sep 20;7(9):73. [Content Brief]
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 and light). 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 | 1.6991 mL | 8.4955 mL | 16.9909 mL | 42.4773 mL |
| 5 mM | 0.3398 mL | 1.6991 mL | 3.3982 mL | 8.4955 mL | |
| 10 mM | 0.1699 mL | 0.8495 mL | 1.6991 mL | 4.2477 mL | |
| 15 mM | 0.1133 mL | 0.5664 mL | 1.1327 mL | 2.8318 mL | |
| 20 mM | 0.0850 mL | 0.4248 mL | 0.8495 mL | 2.1239 mL | |
| 25 mM | 0.0680 mL | 0.3398 mL | 0.6796 mL | 1.6991 mL | |
| 30 mM | 0.0566 mL | 0.2832 mL | 0.5664 mL | 1.4159 mL | |
| 40 mM | 0.0425 mL | 0.2124 mL | 0.4248 mL | 1.0619 mL | |
| 50 mM | 0.0340 mL | 0.1699 mL | 0.3398 mL | 0.8495 mL | |
| 60 mM | 0.0283 mL | 0.1416 mL | 0.2832 mL | 0.7080 mL | |
| 80 mM | 0.0212 mL | 0.1062 mL | 0.2124 mL | 0.5310 mL | |
| 100 mM | 0.0170 mL | 0.0850 mL | 0.1699 mL | 0.4248 mL |
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