Home Protein Tyrosine Kinase EGFR inhibitor BI-4020 For research use only.

BI-4020

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.

BI-4020 Chemical Structure

BI-4020 Chemical Structure

CAS: 2664214-60-0

Purity & Quality Control

Batch: S892101 Ethanol] 30 mg/mL] false] Water] 20 mg/mL] false] DMSO] 15 mg/mL] false Purity: 99.31%
99.31

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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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models NMRI mice
Dosages 10 mg/kg; 1 mg/kg
Administration Oral gavage; IV

Chemical Information & Solubility

Molecular Weight 542.68 Formula

C30H38N8O2
CAS No. 2664214-60-0 SDF --
Smiles CC1CCCOC2=C(C=N[N]2C)C3=NC(=CC(=C3)C(=O)N=C4NC5=C(C=C(CN6CCN(C)CC6)C=C5)N4C1)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

Ethanol : 30 mg/mL

Water : 20 mg/mL

DMSO : 15 mg/mL ( (27.64 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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

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