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BI-4020

Catalog No. T10534   CAS 2664214-60-0

BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. BI-4020 exhibits activity agains the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines), the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM) and EGFR wt (IC50=190 nM). BI-4020 exhibits high kinome selectivity and good DMPK properties.

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BI-4020 Chemical Structure
BI-4020, CAS 2664214-60-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 288.00
5 mg In stock $ 697.00
10 mg In stock $ 996.00
25 mg In stock $ 1,490.00
50 mg In stock $ 1,990.00
1 mL * 10 mM (in DMSO) In stock $ 851.00
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Purity: 100.00%
Purity: 98.44%
ee: 100%
Purity: 97.21%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. BI-4020 exhibits activity agains the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines), the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM) and EGFR wt (IC50=190 nM). BI-4020 exhibits high kinome selectivity and good DMPK properties.
Targets&IC50 EGFRWT:190 nM, EGFRdel19 T790M C797S:0.2 nM, EGFRdel19:1 nM
In vitro BI-4020 inhibits p-EGFR del19 T790M C797S ( IC50: 0.6 nM). 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.
In vivo In the human PC-9 (EGFR del19/T790M/C797S) triple mutant NSCLC xenograft model in mice, BI-4020 leads to tumor regressions.
Molecular Weight 542.68
Formula C30H38N8O2
CAS No. 2664214-60-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 240 mg/mL (442.25 mM), sonification is recommended.

TargetMolReferences and Literature

1. Engelhardt H,et al. Start selective and rigidify: The discovery path towards a next generation of EGFR tyrosine kinase inhibitors. J Med Chem. 2019 Nov 5.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Anti-Pancreatic Cancer Compound Library Orally Active Compound Library Bioactive Compound Library Inhibitor Library Anti-Breast Cancer Compound Library Anti-Lung Cancer Compound Library Macrocyclic Compound Library Anti-Cancer Compound Library Anti-Ovarian Cancer Compound Library

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Keywords

BI-4020 2664214-60-0 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR HER1 inhibit BI4020 BI 4020 Epidermal growth factor receptor ErbB-1 Inhibitor inhibitor

 

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