| Description | Opnurasib (JDQ-443) is an orally available and selective and potent covalent KRAS G12C inhibitor with antitumor activity for the study of advanced non-small cell lung cancer. |
| In vitro | Opnurasib selectively forms a covalent bond with and inhibits GDP-bound KRASG12C, demonstrating a low reversible binding affinity to the RAS switch II pocket. Additionally, it effectively hinders the proliferation of cell lines carrying KRASG12C mutations, as well as those with double mutations G12C/H95, G12C/R68S, and G12C/Y96.[2]Opnurasib induces dose-dependent decreases in phosphorylated ERK (pERK) levels and inhibits the proliferation of KRASG12C-mutated cell lines NCI-H358 and NCI-H2122, exhibiting IC50 values of 0.018 and 0.063 μM, respectively.[2] |
| In vivo | Opnurasib elicits distinct antitumor responses in patient-derived xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal tumors, and these responses are further enhanced when Opnurasib is used in combination with other therapeutic agents.[2] |
| Synonyms | NVP-JDQ443, JDQ-443, Opnurasib |
| molecular weight | 526.03 |
| Molecular formula | C29H28ClN7O |
| CAS | 2653994-08-0 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 70 mg/mL (133.07 mM), Sonication is recommended. |
| References | 1. LIU BO, et al. PYRAZOLYL DERIVATIVES USEFUL AS ANTI-CANCER AGENTS. WO2021120890A1. 2. Weiss A, et al. Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C. Cancer Discov. 2022 Jun 2;12(6):1500-1517. |