Silevertinib
Based on 3 publication(s) in Google Scholar
Silevertinib (BDTX-1535) is an irreversible, brain-penetrant, selective and orally active EGFR inhibitor with wild-type EGFR-sparing. Silevertinib targets key EGFR resistance mutations, including the kinase domain (C797S, L718Q, G724S, S768I), extracellular domain (EGFRvIII, A289X), and EGFR amplification. Silevertinib exerts anti-tumor activity with well tolerated in vivo. Silevertinib can be used for non-small cell lung cancer (NSCLC) and glioblastoma (GBM) research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.74%
- No. CAS: 2607829-38-7
- Fòrmula: C30H30ClFN6O2
- Peso molecular:561.05
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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
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Publications Citing Use of MedChemExpress (MCE) Silevertinib
MoreVer todos los productos específicos de isoformas EGFR
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
C797S |
L718Q |
G724S |
S768I |
A289X |
EGFRvIII |
In Vitro
In Vivo
Silevertinib shows a central nervous system (CNS) Kpuu of 0.55 and 0.48 in rat and dog, respectively[2].
Silevertinib is active in an intracranial PDX model[2].
Silevertinib (o.p., once) suppresses phosphorylation of EGFR mutants for greater than 24h[3].
Silevertinib achieves a broad antitumor efficacy across NsCLC/GBM PDX tumors expressing a family of EGFR oncogenic mutations[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2607829-38-7
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Appearance Solid
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Peso molecular 561.05
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Fòrmula C30H30ClFN6O2
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Color Light yellow to yellow
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SMILES
O=C(/C=C/CN1CCOCC1)NC2=CC3=C(N=CN=C3NC4=C(C(Cl)=CC=C4)F)C=C2C#C[C@]56[C@](CN(C6)C)([H])C5
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Synonyms
BDTX-1535; EGFR-IN-76
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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 (3)
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Journal Impact Factor
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Most Recent
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Cancer Res
Enozertinib is a Selective, Brain-penetrant EGFR inhibitor for Treating Non-small Cell Lung Cancers with EGFR Exon 20 and Atypical Mutations. [Abstract]2025 Nov 6. PMID: 41196054 -
Redox Biol
C-terminal interleukin 1 alpha (IL-1α) overexpression drives EMT and a vulnerability to ferroptosis in HNSCC. [Abstract]2026 Jun:93:104172. PMID: 42013543 -
Cancer Lett
2025 Dec 1:634:218069. PMID: 41033606
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (178.24 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)
In Vivo:
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 (4.46 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.
In Vivo Dissolution Calculator
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 (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 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 | 1.7824 mL | 8.9119 mL | 17.8237 mL | 44.5593 mL |
| 5 mM | 0.3565 mL | 1.7824 mL | 3.5647 mL | 8.9119 mL | |
| 10 mM | 0.1782 mL | 0.8912 mL | 1.7824 mL | 4.4559 mL | |
| 15 mM | 0.1188 mL | 0.5941 mL | 1.1882 mL | 2.9706 mL | |
| 20 mM | 0.0891 mL | 0.4456 mL | 0.8912 mL | 2.2280 mL | |
| 25 mM | 0.0713 mL | 0.3565 mL | 0.7129 mL | 1.7824 mL | |
| 30 mM | 0.0594 mL | 0.2971 mL | 0.5941 mL | 1.4853 mL | |
| 40 mM | 0.0446 mL | 0.2228 mL | 0.4456 mL | 1.1140 mL | |
| 50 mM | 0.0356 mL | 0.1782 mL | 0.3565 mL | 0.8912 mL | |
| 60 mM | 0.0297 mL | 0.1485 mL | 0.2971 mL | 0.7427 mL | |
| 80 mM | 0.0223 mL | 0.1114 mL | 0.2228 mL | 0.5570 mL | |
| 100 mM | 0.0178 mL | 0.0891 mL | 0.1782 mL | 0.4456 mL |
Silevertinib Related Classifications
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