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BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. It exhibits activity against 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 also shows high kinome selectivity and good DMPK properties.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $173 | In Stock | |
5 mg | $418 | In Stock | |
10 mg | $598 | In Stock | |
25 mg | $893 | In Stock | |
50 mg | $1,190 | In Stock | |
100 mg | $1,590 | In Stock | |
200 mg | $2,170 | In Stock | |
1 mL x 10 mM (in DMSO) | $497 | In Stock |
Description | BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. It exhibits activity against 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 also shows high kinome selectivity and good DMPK properties. |
Targets&IC50 | EGFR (T790M/C797S/del19):0.2 nM, EGFR (del19):1 nM, EGFR (WT):190 nM |
In vitro | BI-4020 inhibits p-EGFR del19 T790M C797S (IC50: 0.6 nM) and the triple mutant EGFR (del19/T790M/C797S) variant (IC50=0.2 nM in BaF3 cell lines), as well as the double mutant EGFR (del19/T790M) and primary mutant EGFR del19 (IC50: 1 nM), with activity against EGFR wt (IC50: 190 nM), and exhibits 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 |
Smiles | C[C@@H]1CCCOc2c(cnn2C)-c2cc(cc(C)n2)C(=O)\N=C2/Nc3ccc(CN4CCN(C)CC4)cc3N2C1 |
Relative Density. | 1.33 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 240 mg/mL (442.25 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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