BI-4732
Based on 1 Customer Validation
BI-4732 is an orally active, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC50 values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.81%
- No. CAS: 2769715-68-4
- Fòrmula: C32H36N10O2
- Peso molecular:592.69
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
In Vitro
BI-4732(1-1000 nM, 72 h) exhibits potent anti-proliferative activity against EGFR_E19del/C797S (IC50 = 6 nM), EGFR_L858R/C797S (IC50 = 213 nM), EGFR_E19del/T790M/C797S (IC50 = 4 nM), and EGFR_L858R/T790M/C797S (IC50 = 15 nM) in Ba/F3 cells[1].
BI-4732(10-100 nM, 6 h) inhibits EGFR and downstream signaling phosphorylation in all EGFR_C797S Ba/F3 cells when combined with Osimertinib (HY-15772)[1].
BI-4732 (1-1000 nM, 72 h) shows potent antiproliferative activity against YU-1182, YU-1097, YUO-143, PC9, and PC9_DC cells, with [1].
values of 73 nM, 3 nM, 5 nM, 14 nM, and 25 nM, respectively[1].
BI-4732 (1-30 nM, 21 days) almost completely prevents clonogenicity in YUX-1024, PC9_DC, YU-1182 and YU-1097 cells when combined with Osimertinib (HY-15772)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:All EGFR_C797S Ba/F3 cells
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Concentration:10, 100 nM combined with Osimertinib
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Incubation Time:6 h
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Result:Reduced the phosphorylation of AKT, ERK, and S6K.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:YU-1097 cells (5 × 106 in 100 µL PBS) were subcutaneously implanted into the flanks of 6-week-old female BALB/c nude mice[1]
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Dosage:2.5, 5, 10, 25 mg/kg or 5 mg/kg combined with Osimertinib (25 mg/kg)
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Administration:p.o. twice daily for 4 weeks
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Result:Achieved tumor growth inhibition (TGI) rates of 143.1%, 154.0%, 174.1%, and 183.2% at doses of 2.5, 5, 10, and 25 mg/kg, respectively.
Showed no significant changes in body weight.
Reduced the Ki67 expression.
Appeared phosphorylation of EGFR and its downstream molecules, AKT, ERK, and S6K after 6 h.
Showed greater tumor regression with 176.2% TGI when combined with Osimertinib.
- Kinase activity and phosphorylation assays
- Western Blot
- Patient-Derived Xenograft (PDX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Protocol for Kinase activity and phosphorylation assays
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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No. CAS 2769715-68-4
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Appearance Solid
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Peso molecular 592.69
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Fòrmula C32H36N10O2
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Color Light yellow to yellow
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SMILES
CC1=C(C=NN2C3=NC(N4C[C@@H]5OC[C@H]4C5)=C6C(N(C)C(N7C[C@@H](CCC8)N8CC7)=N6)=C3)C2=CC(C9=C(OC)C=CN=C9)=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
In Vitro:
DMSO : 2 mg/mL (3.37 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 (protect from 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 (protect from light). 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 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.
Working solution concentration: 0.22 mg/mL
Pureza y Documentación
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Ficha de datos (279 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
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 (protect from 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6872 mL | 8.4361 mL | 16.8722 mL | 42.1806 mL |
BI-4732 Related Classifications
HY-161275 Related Classifications
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