| Description | Divarasib (GDC-6036) (GDC-6036) is an investigational, oral, high-potency and selective KRAS G12C inhibitor with an IC50 of < 0.01 μM. Divarasib irreversibly locks KRAS G12C oncoprotein in an inactive state and inhibits tumor cell growth. It is being investigated for use in solid tumors, including non-small cell lung and colorectal cancers and other types of cancer. |
| In vitro | Divarasib exhibits a potency with an EC50 value of 2 nM in K-Ras G12C-alkylation HCC1171 cells.[2] |
| In vivo | Administration of Divarasib (10-100 mg/kg/day; PO for 7 days) results in a reduction in the ratio of free KRAS G12C.[1] |
| Target activity | KRas (G12C):<0.01 μM |
| Synonyms | GDC-6036 |
| molecular weight | 622.06 |
| Molecular formula | C29H32ClF4N7O2 |
| CAS | 2417987-45-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 90.0 mg/mL (144.7 mM), Sonication is recommended. |
| References | 1. Meng L, et al. Assessment of KRAS G12C Target Engagement by a Covalent Inhibitor in Tumor Biopsies Using an Ultra-Sensitive Immunoaffinity 2D-LC-MS/MS Approach. Anal Chem. 2022;94(37):12927-12933. 2. Sushant Malhotra, et al. Fused ring compounds. WO2020097537A2. 3. Tran JC, et al. Quantifying KRAS G12C Covalent Drug Inhibitor Activity in Mouse Tumors Using Mass Spectrometry. Anal Chem. 2023;95(11):4834-4839. |