| Bioactivity | EGFR-IN-44 (Compound 6a) is a potent, orally active EGFR tyrosine kinase inhibitor with an IC50 of 4.11 nM. EGFR-IN-44 induces cell apoptosis and shows an oral bioavailability value of 33.57%. EGFR-IN-44 can be studied for non-small-cell lung cancers[1]. |
| Target | IC50: 0.26 nM (EGFR T790M/L858R), 1.33 nM (EGFR L858R), 4.11 nM (EGFR) |
| Invitro | EGFR-IN-44 (Compound 6a) (0-10 µM, 72 h) shows anti-proliferative activities against tumor cell lines[1]. EGFR-IN-44 binds to the ATP binding site of EGFR[1].EGFR-IN-44 (0-10 nM, 48 h) induces H1975 cell apoptosis via the mitochondrial pathway, arrests cell cycle in G0/G1 phase, and suppresses cell migration[1].EGFR-IN-44 (0-10 nM, 48 and 72h) shows hypotoxicity against normal cells[1]. Cell Proliferation Assay[1] Cell Line: |
| In Vivo | EGFR-IN-44 (Compound 6a) (25 mg/kg; i.g.; daily, 7days) shows strong antitumor activity without obvious toxicity[1]. Animal Model: |
| Name | EGFR-IN-44 |
| Formula | C27H29ClN6O2S |
| Molar Mass | 537.08 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Baijiao An, et al. Novel third-generation pyrimidines-based EGFR tyrosine kinase inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer. Bioorg Chem. 2022 May;122:105743. |