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BI-4020
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.
Catalog No. T10534Cas No. 2664214-60-0
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Purity:100.00%
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BI-4020
Catalog No. T10534Cas No. 2664214-60-0
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.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | 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 |
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CitedProduct Introduction
Bioactivity
Chemical Properties
| 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 |
Storage & Solubility Information
| 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 | ||||||||||||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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