| Name | Opnurasib |
| 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] |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 70 mg/mL (133.07 mM), Sonication is recommended.
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| Keywords | JDQ 443 | NVP-JDQ-443 | NVP-JDQ 443 | JDQ443 |
| Inhibitors Related | Adagrasib | (S)-AMG-510 | BI-2493 | CCG-257081 | Ketoconazole | Deltarasin | MRTX1133 | Salirasib | RMC-6236 | (S)-(-)-Perillyl alcohol | CASIN | Sotorasib |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Drug Repurposing Compound Library | Bioactive Compounds Library Max | GPCR Compound Library |
United States
