BI-4020

Catalog No.S8921 Batch:S892101

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Technical Data

Formula

C30H38N8O2
Molecular Weight 542.68 CAS No. 2664214-60-0
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)
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.75mg/ml Taking the 1 mL working solution as an example, add 50 μL of 15 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
0.75mg/ml Taking the 1 mL working solution as an example, add 50 μL of 15 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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 (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    NMRI mice

  • Dosages

    10 mg/kg; 1 mg/kg

  • Administration

    Oral gavage; IV

Selleck's BI-4020 has been cited by 1 publication

Potential Utility of a 4th-Generation EGFR-TKI and Exploration of Resistance Mechanisms-An In Vitro Study [ Biomedicines, 2024, 12(7)1412] PubMed: 39061985

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.