Pan-RAS-IN-6 

Pan-RAS-IN-6 (compound 24) is an inhibitor targeting DUSP6, which reduces MAPK activation in the brain of the NCI-H1373-Luc model (DUSP6), at the same time, it shows significant tumor growth inhibition and tumor regression effects in the NSCLC brain metastasis mouse model. Pan-RAS-IN-6 shows high selectivity and strong inhibitory effects, especially in KRAS mutation-related signaling pathways, demonstrating varying inhibitory activity against different KRAS mutants and interacting proteins. The IC₅₀ values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively^[1].

Pan-RAS-IN-6 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]。
Pan-RAS-IN-6 对 KRAS G12V、野生型 KRAS、野生型 HRAS、野生型 NRAS-BRAF 与 CYPA 相互作用的 IC₅₀ 分别为 7 nM, 32 nM, 38 nM 和 35 nM; 在 G12C、G12D 和 G12V 条件下，对 KRAS-BRAF 与 CYPA 相互作用的 IC₅₀ 分别为 9.7 nM, 49.5 nM 和 7.1 nM; 抑制 pERK 时，对 G12C 和 G12V 的 IC₅₀ 均小于 0.6 nM，而对 G12D 的 IC₅₀ 为 0.9 nM^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Pan-RAS-IN-6 (30 mg/kg，p.o.，每日一次) 在非小细胞肺癌 (NSCLC) 脑肿瘤小鼠模型中抑制肿瘤生长，促进肿瘤消退^[1]。
Pan-RAS-IN-6 (30 mg/kg，p.o.，每日一次) 降低了 NCI-H1373-Luc 模型大脑中 DUSP6 的表达^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

837.08

C₄₆H₆₀N₈O₅S

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Jianguo Chen, et al. Design, Tricyclic compounds for the treatment of cancer. WO2024169914A1. 2024-02-08