BDTX-189 (C09-0786-035)

InformationBDTX-189 is a potent and selective inhibitor of allostericEGFRandHER2oncogenic mutations with Kd of 0.2 nM, 0.76 nM, 13 nM and 1.2 nM for EGFR, HER2,BLKandRIPK2, reapectively. BDTX-189 exhibits anticancer activity.TargetsEGFR (Cell-free assay); HER2 (Cell-free assay); RIPK2 (Cell-free assay); BLK (Cell-free assay) 0.2 nM(Kd); 0.76 nM(Kd); 1.2 nM(Kd); 13 nM(Kd)In vitroBDTX-189 is a potent, selective, irreversible active site inhibitor of the ERBB allosteric mutant oncogene family. BDTX-189 achieves a superior selectivity profile in cell-based assays.In vivoBDTX-189 is differentiated by potent, sustained inactivation of multiple allosteric ERBB mutants in vivo. BDTX-189 achieves dose-dependent regression of allosteric HER2 and EGFR tumors at well-tolerated doses.Cell Research(from reference)Cell lines：A431 cells, H292 cells Incubation Time：0-24 h. Specification: 0.98 Molecular Formula: C29H29ClN6O4 Molecular Weight: 561.03 PubChem CID: 154824631 Isomeric SMILES: C=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)OCCN5CCOCC5