BPI-361175
BPI-361175 is an orally active and blood-brain barrier-penetrant EGFR inhibitor. BPI-361175 inhibits EGFR tyrosine kinase activity and exhibits higher selectivity for mutant EGFR over wild-type EGFR. BPI-361175 can be used for research on non-small cell lung cancer.
For research use only. We do not sell to patients.
- CAS No.: 2595202-07-4
- Formula: C30H37BrN7O3P
- Molecular Weight:654.54
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All EGFR Isoforms
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Biological Activity
Description
In Vitro
BPI-361175 (0.7-465 nM) inhibits Ba/F3-EGFR-19del/T790M/C797S-TK and Ba/F3-EGFR-L858R/T790M/C797S-TK with IC50 values of 0.7 nM and 3.6 nM, respectively, while showing reduced wild-type EGFR activity (IC50 = 465 nM)[1].
BPI-361175 potently inhibits EGFR kinase activity across triple, double, and single EGFR mutant forms (EGFRdel19 or L858R/T790M/C797S; EGFRdel19 or L858R/T790M; EGFRdel19 or L858R/C797S; EGFRdel19; EGFRL858R) while showing no activity against EGFRWT and IGF1R in cell-free assays[2].
BPI-361175 dose-dependently inhibits EGFR phosphorylation and proliferation in cell lines harboring triple, double, and single EGFR mutations (EGFRdel19 or L858R/T790M/C797S; EGFRdel19 or L858R/T790M; EGFRdel19 or L858R/C797S; EGFRdel19; EGFRL858R) and lacks activity against EGFRWT and IGF1R in cell-based assays[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2595202-07-4
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Molecular Weight 654.54
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Formula C30H37BrN7O3P
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SMILES
CCN1C=C(C=N1)C2=CC(NC3=NC(NC4=CC=C(C(C)=C4P(C)(C)=O)C)=C(C=N3)Br)=C(C=C2N5CCOCC5)OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)