Theliatinib 是一种ATP 竞争性高度选择性的EGFR 抑制剂，Ki 为 0.05 nM，IC50为 3 nM。它具有抗肿瘤活性，对EGFR T790M/L858R 突变体的IC50值为 22 nM。它对EGFR 的选择性是其他激酶的 50 倍以上。 Targets WT EGFR (Cell-free assay); EGFR T790M/L858R (Cell-free assay) 3 nM; 22 nM In vitro In comparison to erlotinib or gefitnib, theliatinib shows much stronger binding affinity to wild type EGFR and is more difficult to be replaced by ATP. This unique feature may result in better target engagement for theliatinib compared to erlotinib or gefitinib, leading to stronger anti-tumor activity in tumors with wild type EGFR activation due to gene amplification or protein overexpression. Theliatinib inhibits EGFR phosphorylation with an IC50 of 0.007 μM for EGF stimulated EGFR phosphorylation in A431 cells and cell survival in tumor cells with wild-type EGFR (A431, H292, FaDu cells). Theliatinib demonstrates dose-dependent anti-tumor activity in a panel of PDECX (patient-derived esophageal cancer xenograft) models with a generally good correlation between EGFR H score and tumor growth inhibition. Furthermore, aberrant activation or gene mutations of other targets such as PI3K and FGFR diminishes the anti-tumor activity of the EGFR TKIs, especially, theliatinib. Cell Research(from reference) Cell lines：A431 cells Concentrations：0.005-10 μM Incubation Time：48 h
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Theliatinib (HMPL-309)
CAS number：1353644-70-8 molecular formula：C25H26N6O2
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| Chinese alias | - | ||
| English alias | SCHEMBL247509 | AC-35865 | s8584 | AKOS032946520 | XILIERTINIB [WHO-DD] | 6ZZ3B7NZ0B | Pyrrolo(3,4-b)pyrrole-5(1H)-carboxamide, N-(4-((3-ethynylphenyl)amino)-7-methoxy-6-quinazolinyl)hexahydro-1-methyl-, (3aR,6aR)- | (3aR,6aR)-N-[4-(3-ethynylanilino)-7-me | ||
| CAS number | 1353644-70-8 | molecular formula | C25H26N6O2 |
| molecular weight | 442.51 g/mol | Exact mass | - |
| PSA | 82.600 Ų | logp | 3.100 |
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