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Pan-RAS-IN-6

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Bioactivity 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].
Invitro 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. 0 --> Pan-RAS-IN-6 相关抗体:
In Vivo 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. 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

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