| Bioactivity | DUSP6-IN-1 (compound 24) is an inhibitor targeting DUSP6, with IC50 values of 1.3 nM, 4.7 nM and 0.3 nM for KRAS G12C, G12D and G12V, respectively; IC50 values of 7 nM, 32 nM, 38 nM and 35 nM for the interaction of KRAS G12V, WT KRAS, WT HRAS and WT NRAS-BRAF with CYPA, respectively; IC50 values of 9.7 nM, 49.5 nM and 7.1 nM for KRAS-BRAF and CYPA under G12C, G12D and G12V, respectively; when inhibiting pERK, IC50 values for G12C and G12V are less than 0.6 nM, andIC50value for G12D is 0.9 nM[1]. |
| Invitro | DUSP6-IN-1 抑制 NCI-H23, NCI-H358, NCI-H2444, RKN, SW620 细胞增殖，IC50 为 0.17 nM，0.12 nM，0.17 nM，0.045 nM，0.1 nM[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> DUSP6-IN-1 相关抗体: |
| In Vivo | DUSP6-IN-1 (30 mg/kg，口服，每日一次) 在脑肿瘤小鼠模型中抑制肿瘤生长，促进肿瘤消退[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C46H60N8O5S |
| Molar Mass | 837.08 |
| 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]. Jianguo Chen, et al. Design, Tricyclic compounds for the treatment of cancer. WO2024169914A1. 2024-02-08 |