BI-4020

For research use only.

Catalog No.S8921

BI-4020 Chemical Structure

CAS No. No

BI-4020 is an orally active, non-covalent EGFR inhibitor with IC50 of 0.6 nM and 0.2 nM for EGFRdel19 T790M C797S as biomarker potency and anti-proliferation potency in BaF3 cells, respectively.

Purity & Quality Control

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Biological Activity

Description BI-4020 is an orally active, non-covalent EGFR inhibitor with IC50 of 0.6 nM and 0.2 nM for EGFRdel19 T790M C797S as biomarker potency and anti-proliferation potency in BaF3 cells, respectively.
Targets
EGFRdel19 T790M C797S [1]
(anti-proliferation potency)
EGFRdel19 T790M C797S [1]
(biomarker potency)
0.2 nM 0.6 nM
In vitro

BI-4020 is a noncovalent, macrocyclic TKI, which inhibits not only the triple mutant EGFRdel19 T790M C797S variant but also the double mutant EGFRdel19 T790M and primary mutant EGFRdel19 while sparing activity against EGFRwt.[1]

In vivo

BI-4020 shows high potency on EGFR mutant cells, high kinome selectivity, and good DMPK properties, which leads to tumor regressions in the human PC-9 (EGFRdel19 T790M C797S) triple mutant NSCLC xenograft model in mice.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: BaF3 cells
  • Concentrations: --
  • Incubation Time: 4 h, 3 days
  • Method:

    Kinase selectivity is determined using the SelectScreen Kinase Profiling Services. The inhibition of the p-EGFRdel19 T790M C797S signal in BaF3 cells is measured after 4 h BI-4020 treatment. BaF3 cells bearing EGFRdel19 T790M C797S protein are treated for 3 days with BI-4020, and the effect on proliferation is measured.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: NMRI mice
  • Dosages: 10 mg/kg; 1 mg/kg
  • Administration: Oral gavage; IV
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 30 mg/mL (55.28 mM)
Water 20 mg/mL (36.85 mM)
DMSO 15 mg/mL (27.64 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 542.68
Formula

C30H38N8O2

CAS No. No
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID