kras inhibitor-10

KRAS inhibitor-10 (WO2021005165 A1, compound 11) is a potent and selective inhibitor of RAS proteins, with a specific focus on KRAS proteins. This orally active anti-cancer agent demonstrates strong efficacy in cancer research, specifically in pancreatic cancer, breast cancer, multiple myeloma, leukemia, and lung cancer. KRAS inhibitor-10 is classified as a tetrahydroisoquinoline compound. Its inhibitory properties provide valuable insights and potential therapeutic applications in the field of oncology [1].

KRas(G12C) inhibitor 6 是一种变构的，选择性的 K-Ras(G12C)抑制剂。

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.

SOS1-IN-10 是一种 SOS1 的有效抑制剂，能够作用于 KRAS G12C-SOS1 (IC50: 13 nM)。

KRAS inhibitor-18 (compound 3-10) 是一种 KRAS G12C 的有效抑制剂 (IC50: 4.74 μM)。KRAS inhibitor-18 在 MIA PaCA-2，A549 细胞中表现出 p-ERK 抑制作用，IC50s 分别为 66.4，11.1 μM。KRAS inhibitor-18 具有潜力进行胰腺癌、结直肠癌和肺癌的研究。

KRAS G12D inhibitor 10 是一种有效的KRAS G12D 抑制剂。Ras 蛋白家族是一种重要的细胞内信号分子，在生长发育中起重要作用。KRAS G12D inhibitor 10 具有研究 KRAS G12D 介导的癌症的潜力。

Pan-KRAS-IN-2（compound 6）是一种抑制剂，对KRAS WT及其多种突变体（G12D、G12C、G12V、G12S、G12A、Q61H）表现出极高的抑制活性，其IC50均不超过10 nM；然而对KRAS G13D的抑制活性较低，IC50超过10 μM。