1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. BI-4020

BI-4020 

Cat. No.: HY-129550
Handling Instructions

BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM). BI-4020 also shows activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties.

For research use only. We do not sell to patients.

BI-4020 Chemical Structure

BI-4020 Chemical Structure

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5 mg USD 350 Ask For Quote & Lead Time
10 mg USD 550 Ask For Quote & Lead Time
50 mg USD 1650 Ask For Quote & Lead Time
100 mg USD 2250 Ask For Quote & Lead Time

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Description

BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM). BI-4020 also shows activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties[1].

IC50 & Target[1]

EGFRdel19 T790M C797S

0.2 nM (IC50)

EGFRdel19

1 nM (IC50)

EGFRWT

190 nM (IC50)

EGFRdel19 T790M

 

In Vitro

BI-4020 inhibits p-EGFR del19 T790M C797S with an IC50 of 0.6 nM[1].

In Vivo

BI-4020 leads to tumor regressions in the human PC-9 (EGFR del19 T790M C797S) triple mutant NSCLC xenograft model in mice[1].

Molecular Weight

542.68

Formula

C₃₀H₃₈N₈O₂

SMILES

O=C(C1=CC(C)=NC(C2=C(OCCC[[email protected]@H](C)C3)N(C)N=C2)=C1)/N=C(N4)/N3C5=C4C=CC(CN6CCN(C)CC6)=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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KeyWords:

BI-4020 | BI4020 | BI 4020 | EGFR | Epidermal growth factor receptor | ErbB-1 | HER1 | Inhibitor | inhibitor | inhibit

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BI-4020
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HY-129550
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