AZD3759 (C007B-021014)

InformationAZD3759 is a potent, oral active, CNS-penetrantEGFRinhibitor withIC50of 0.3 nM, 0.2 nM, and 0.2 nM for EGFR (WT), EGFR (L858R), and EGFR (exon 19Del), respectively. Phase 1.TargetsEGFR (L858R) (Cell-free assay); EGFR (exon 19Del) (Cell-free assay); EGFR (WT) (Cell-free assay) 0.2 nM; 0.2 nM; 0.3 nMIn vitroIn H3255 (L858R) cells, AZD3759 inhibits EGFR phosphorylation with IC50 of 7.2 nM. AZD3759 demonstrates inhibitory effects on both the pEGFR pathway and cell proliferation of EGFR mutation-derived cells PC-9 and H3255 with IC50 of 7.7 nM and 7 nM, respectively, showing mo activity on cell proliferation of H838 cells.In vivoAZD3759 shows good oral bioavailability in dogs, and penetrates extensively into monkey brain. In a brain metastasis PC-9 (Exon19Del) model, AZD3759 (15 mg/kg) causes significant dose-dependent antitumor efficacy.Cell Research(from reference)Cell lines：PC-9 (exon 19Del), H3255 (L858R) and H838 (wt) cells Concentrations：~30 mM Incubation Time：72 h. Specification: 0.99 Molecular Formula: C22H23ClFN5O3 Molecular Weight: 459.9 PubChem CID: 78209992 Isomeric SMILES: C[C@@H]1CN(CCN1C(=O)OC2=C(C=C3C(=C2)C(=NC=N3)NC4=C(C(=CC=C4)Cl)F)OC)C Related Documents: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/A413895-SCI_7882742d5fa7b3cde1b4b24d170b216f.pdf