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).
For research use only. We do not sell to patients.
- Purity: 99.30%
- CAS No.: 2769715-68-4
- Formula: C32H36N10O2
- Molecular Weight:592.69
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All EGFR Isoforms
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Biological Activity
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.
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.
Chemical Information
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CAS No. 2769715-68-4
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Appearance Solid
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Molecular Weight 592.69
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
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)
Purity & Documentation
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Data Sheet (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)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 |
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