Befotertinib
Based on 2 publication(s) in Google Scholar
Befotertinib (D-0316) is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib selectively targets EGFR mutations including EGFRT790M, EGFRL858R and delE746-A750, forms covalent bonds with EGFRC797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib can be used in research related to multidrug-resistant cancers and non-small cell lung cancer.
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- Pureza: 99.86%
- No. CAS: 1835667-63-4
- Fòrmula: C29H32F3N7O2
- Peso molecular:567.61
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Almacenamiento:Powder -20°C, 3 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
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Publications Citing Use of MedChemExpress (MCE) Befotertinib
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Actividad biológica
Befotertinib (0.1-100 μM; 72 h) exhibits comparable cytotoxic activity in ABCB1-overexpressing KB-V1, NCI-ADR-RES, MDR19-HEK293 cells and their parental cell lines KB-3-1, OVCAR-8, pcDNA3.1-HEK293[1].
Befotertinib (2 μM; 48 h) enhances Paclitaxel (HY-B0015)-induced apoptosis. After 48 h of combined treatment, the proportion of apoptotic cells increases to 85% in KB-V1 cells and to 95% in NCI-ADR-RES cells[1].
Befotertinib (10 μM; 10 min) inhibits ABCB1-mediated drug efflux and significantly enhances calcein accumulation in KB-V1, NCI-ADR-RES and MDR19-HEK293 cells after 10 minutes of incubation[1].
Befotertinib (0.001-10000 nM; 72 h) potently inhibits the proliferation of EGFR-mutant non-small cell lung cancer (NSCLC) cell lines H1975, HCC-827 and H3255, with EC50 values of 1.2 nM, 3.0 nM and 4.3 nM, respectively; whereas it exerts minimal effects on A431 cells overexpressing wild-type (WT) EGFR, with an EC50 value of 1200 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KB-V1, NCI-ADR-RES
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Concentration:2 μM (befotertinib); 1 μM (paclitaxel)
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Incubation Time:48 h
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Result:Induced minimal apoptosis (apoptotic cell populations below 10%) when treated alone in KB-V1 and NCI-ADR-RES cells.
Increased apoptosis to 85% in KB-V1 cells and almost 95% in NCI-ADR-RES cells when co-treated with paclitaxel, comparable to the positive control combination of tariquidar and paclitaxel.
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Cell Line:HCC-827 (delE746-A750), H3255 (L858R), H1975 (L858R/T790M), A431 (WT EGFR overexpressing)
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Concentration:0.001-10000 nM
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Incubation Time:72 h
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Result:Exhibited an antiproliferative EC50 of 1200 nM against A431 WT EGFR-overexpressing cells.
Exhibited an antiproliferative EC50 of 1.2 nM against H1975 L858R/T790M EGFR cells.
Exhibited an antiproliferative EC50 of 3.0 nM against HCC-827 delE746-A750 EGFR cells.
Exhibited an antiproliferative EC50 of 4.3 nM against H3255 L858R EGFR cells.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1835667-63-4
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Appearance Solid
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Peso molecular 567.61
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Fòrmula C29H32F3N7O2
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC(NC2=NC(C3=CN(CC(F)(F)F)C4=C3C=CC=C4)=CC=N2)=C(C=C1N(CCN(C)C)C)OC)C=C
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Synonyms
D-0316
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 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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J Med Chem
2025 Aug 28;68(16):17917-17932. PMID: 40801664 -
Solvente y solubilidad
DMSO : 50 mg/mL (88.09 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.
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 (3.66 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 (281 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Li YC, et al. Befotertinib restored chemosensitivity to multidrug-resistant cancer cells by inhibiting the drug efflux activity of ABCB1. J Pharm Pharmacol. 2026;78(3):rgag020. [Content Brief]
[2]. Damghani T, et al. Profiling and Optimizing Targeted Covalent Inhibitors through EGFR-Guided Studies. J Med Chem. 2025;68(16):17917-17932. [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. 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 | 1.7618 mL | 8.8089 mL | 17.6177 mL | 44.0443 mL |
| 5 mM | 0.3524 mL | 1.7618 mL | 3.5235 mL | 8.8089 mL | |
| 10 mM | 0.1762 mL | 0.8809 mL | 1.7618 mL | 4.4044 mL | |
| 15 mM | 0.1175 mL | 0.5873 mL | 1.1745 mL | 2.9363 mL | |
| 20 mM | 0.0881 mL | 0.4404 mL | 0.8809 mL | 2.2022 mL | |
| 25 mM | 0.0705 mL | 0.3524 mL | 0.7047 mL | 1.7618 mL | |
| 30 mM | 0.0587 mL | 0.2936 mL | 0.5873 mL | 1.4681 mL | |
| 40 mM | 0.0440 mL | 0.2202 mL | 0.4404 mL | 1.1011 mL | |
| 50 mM | 0.0352 mL | 0.1762 mL | 0.3524 mL | 0.8809 mL | |
| 60 mM | 0.0294 mL | 0.1468 mL | 0.2936 mL | 0.7341 mL | |
| 80 mM | 0.0220 mL | 0.1101 mL | 0.2202 mL | 0.5506 mL |
Befotertinib Related Classifications
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