| Bioactivity | MAPK-IN-2 (compound 3h) is a potent MAPK inhibitor with antineoplastic activity. MAPK-IN-2 inhibits cancer cell proliferation among serval cancer cell lines, and suppresses MAPK pathway with potant efficacy (EGFRWT IC50=281 nM, c-MET IC50=205 nM, B-RAFWT IC50=112 nM, and CDK4/6 IC50=95 and 184 nM, respectively). MAPK-IN-2 even shows a remarkable potency against mutated EGFR and B-RAF (EGFRT790M IC50=69 nM and B-RAFV600E IC50=83 nM)[1]. |
| Target | IC50: 281 nM (EGFRWT), 69 nM (EGFRT790M), 205 nM (c-MET), 112 nM (B-RAFWT), 83 nM (B-RAFV600E), 95 nM (CDK4), 184 nM (CDK6) |
| Name | MAPK-IN-2 |
| Formula | C20H11Cl2N3O |
| Molar Mass | 380.23 |
| 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]. Saleh MM, et al. The mystery of titan hunter: Rationalized striking of the MAPK pathway via Newly synthesized 6-Indolylpyridone-3-Carbonitrile derivatives. Eur J Med Chem. 2023 Nov 5;259:115675. |