| Name | BI-4142 |
| Description | BI-4142 is an orally active, potent and selective HER2 inhibitor that inhibits cancer cell proliferation, suppresses her2-dependent cell lines and inhibits downstream signalling. |
| In vitro | BI-4142 inhibits HER2-dependent cell lines and downstream signaling, with IC50 values of 10 nM, 18 nM, 270 nM, and 2400 nM against HEK HER2YVMA, Ba/F3 HER2YVMA, HEK EGFRWT, and Ba/F3 EGFRWT, respectively[1].BI-4142 (1 nM-5 μM, 72 h or 96 h) exhibits antiproliferative activity against tumor cells[1].
In the CaCo-2 assay, BI-4142 displays good permeability and no PgP-mediated efflux liability[1]. |
| In vivo | BI-4142 administered at doses ranging from 0 to 100 mg/kg, orally twice daily for 40 days, significantly inhibits tumor growth and suppresses oncogenic signaling[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 80 mg/mL (153.38 mM), Sonication is recommended.
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| Keywords | HER2 |
| Inhibitors Related | (S)-Afatinib | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Erlotinib hydrochloride | Erlotinib | Neratinib | Afatinib | Chalcone | Brigatinib | Genistein | Gefitinib |
| Related Compound Libraries | Anti-Lung Cancer Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Ovarian Cancer Compound Library | Inhibitor Library | Stem Cell Differentiation Compound Library | Orally Active Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |