Sevabertinib
Based on 1 Customer Validation
Sevabertinib (BAY 2927088) is an orally active and reversible dual EGFR-HER2 inhibitor (IC50 <0.5 nM for wild-type HER2, HER2 A775insYVMA, wild-type EGFR, and EGFR D770_N771insSVD). Sevabertinib has anticancer activity against lung cancer.
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- Pureté: 99.90%
- CAS No.: 2521285-05-0
- Formule: C24H25ClN4O5
- Masse moléculaire:484.93
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
IC50: <0.5 nM for wild-type HER2, HER2 A775insYVMA, wild-type EGFR, and EGFR D770_N771insSVD[2]
Sevabertinib exhibits an IC50 of <0.5 nM against wild-type HER2, HER2 A775insYVMA, wild-type EGFR, and EGFR D770_N771insSVD at a physiological ATP concentration of 2 mM, and shows significantly reduced activity against HER4 (IC50 = 13.9 nM)[2].
Sevabertinib potently inhibits the proliferation of isogenic Ba/F3 cells ectopically expressing HER2 exon 20 insertions, activating HER2 point mutations, or putative secondary acquired resistance mutations (T798M, T798I, C805S)[2].
Sevabertinib potently inhibits the proliferation of two lung cancer cell lines: NCI-H1781 (harboring HER2 exon 20 insertion mutations A775insV and G776C) with an IC50 of 19.7 nM, and NCI-H2170 (harboring wild-type ERBB2 amplification) with an IC50 of 16.7 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Sevabertinib (5-10 mg/kg; p.o.; twice daily for 5 mg/kg; once daily for 10 mg/kg) demonstrates antitumor efficacy in the NCI-H1781 xenograft mouse model, with similar efficacy to Zongertinib (HY-148810)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice + subcutaneous CTG-2543 PDX NSCLC model (HER2 A775insYVMA)[2]
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Dosage:10 mg/kg, 25 mg/kg, 50 mg/kg
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Administration:Oral gavage, once daily (QD)
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Result:Showed T/C ratios of 0.22, 0.12, and 0.06 at doses of 10 mg/kg, 25 mg/kg, and 50 mg/kg, respectively.
Was well-tolerated as no marked body weight loss was observed.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2521285-05-0
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Appearance Solid
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Masse moléculaire 484.93
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Formule C24H25ClN4O5
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Color Light yellow to yellow
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SMILES
O=C(NCC1)C2=C1NC(C3=CC=NC=C3OC[C@@H]4COCCO4)=C2NC5=C(C(Cl)=CC=C5)OC
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Synonyms
BAY 2927088
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 50 mg/mL (103.11 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)
Pureté et documentation
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Fiche technique (278 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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Instruction de manipulation (2659 KB)
Références
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 | 2.0622 mL | 10.3108 mL | 20.6215 mL | 51.5538 mL |
| 5 mM | 0.4124 mL | 2.0622 mL | 4.1243 mL | 10.3108 mL | |
| 10 mM | 0.2062 mL | 1.0311 mL | 2.0622 mL | 5.1554 mL | |
| 15 mM | 0.1375 mL | 0.6874 mL | 1.3748 mL | 3.4369 mL | |
| 20 mM | 0.1031 mL | 0.5155 mL | 1.0311 mL | 2.5777 mL | |
| 25 mM | 0.0825 mL | 0.4124 mL | 0.8249 mL | 2.0622 mL | |
| 30 mM | 0.0687 mL | 0.3437 mL | 0.6874 mL | 1.7185 mL | |
| 40 mM | 0.0516 mL | 0.2578 mL | 0.5155 mL | 1.2888 mL | |
| 50 mM | 0.0412 mL | 0.2062 mL | 0.4124 mL | 1.0311 mL | |
| 60 mM | 0.0344 mL | 0.1718 mL | 0.3437 mL | 0.8592 mL | |
| 80 mM | 0.0258 mL | 0.1289 mL | 0.2578 mL | 0.6444 mL | |
| 100 mM | 0.0206 mL | 0.1031 mL | 0.2062 mL | 0.5155 mL |
Sevabertinib Related Classifications
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