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Cat. No.: HY-189685

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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.

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CAS No.: 2595202-07-4
Formule: C₃₀H₃₇BrN₇O₃P
Masse moléculaire:654.54

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Please store the product under the recommended conditions in the Certificate of Analysis.

BPI-361175 Chemical Structure

CAS No.: 2595202-07-4

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Activité biologique
- Description
- In Vitro
Chemical Information
Pureté et documentation
Références
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Activité biologique

Description

Voir tous les produits spécifiques à Isoform EGFR :

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.

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Chemical Information

CAS No. 2595202-07-4
Masse moléculaire 654.54
Formule C₃₀H₃₇BrN₇O₃P
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Kadam VM, et al. Recent advances in synthetic strategies of fourth-generation EGFR tyrosine kinase inhibitors under clinical trials for the treatment of resistant non-small cell lung cancer (NSCLC). Bioorganic chemistry. 2026 Oct 05;181:110353.

[2]. Liu L, e al. Abstract 5462: BPI-361175, a 4th generation EGFR-TKI for the treatment of non-small cell lung cancer (NSCLC). Cancer Res. 2022;82(12_Supplement):5462.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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