kras g12c inhibitor 15

KRAS G12C inhibitor 15 is a potent KRAS G12C inhibitor .

KRASG12C IN-14（化合物15）作为针对KRAS基因G12C突变的抑制剂, 显示出对CYPA依赖的KRAS-BRAF具有抑制作用，其IC50值为0.002 μM。此外，该化合物在NCI-H358细胞中对ERK磷酸化的抑制作用IC50同样为0.002 μM。

RAS RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS RAS-RAF-IN-1 has a KD of 5.0 μμ-15 μμ for cyclophilin A (CYPA) binding affinity. RAS RAS-RAF-IN-1 has antitumor activity[1]. RAS RAS-RAF-IN-1 (compound 89; for 4 hours) has an EC50 of 0.5 μμ-5.0 μμ for BRAF-GTP-KRAS-G12C disruption and has an IC50 of 1.0 μμ-10 μμ for pERK inhibition in H358 cells[1]. [1]. Meizhong Jin, et al. Compounds that participate in cooperative binding and uses thereof. WO2020132597A1.

KRAS inhibitor-15 (compound 3-19) 是一种 KRAS G12C 的有效抑制剂 (IC50: 0.954 μM)。KRAS inhibitor-15 在 MIA PaCA-2，A549 细胞中表现出 p-ERK 抑制作用，IC50s 分别为 2.03，>33.3 μM。KRAS inhibitor-15 具有潜力进行胰腺癌、结直肠癌和肺癌的研究。