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BI-4020

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SI-7829

BI-4020, >98% (HPLC)

CAS No. : [2664214-60-0]

IUPAC Name : (R,E)-11,26,7-Trimethyl-56-((4-methylpiperazin-1-yl)methyl)-52,53-dihydro-11H,51H-11-oxa-4-aza-5(2,1)-benzo[d]imidazola-2(2,4)-pyridina-1(4,5)-pyrazolacycloundecaphan-3-one

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Chemical Properites
Mol. Formula :
C30H38N8O2
Mol. Weight :
542.69
Appearance :
Solid
Melting Point :
Not available
For Laboratory research use only, not for drug, household or other uses.

Applications : 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.

References : Engelhardt H. et al.: J. Med. Chem., 62(22), 10272-10293, 2019.

Storage : Keep container tightly closed under nitrogen or argon and refrigerate for long-term shelf life.

Caution : In case of contact with skin or eyes, rinse immediately with plenty of water and seek medical advice. Wear suitable protective clothing and gloves.

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