| Description | RMC-6236 is a RAS(ON)MULTI inhibitor with anticancer activity and is used in the study of advanced malignant solid tumors and colorectal cancer. |
| In vitro | 方法：使用RMC-6236（1，3，10，30nM，4h）处理HPAC和Capan-2细胞系，观察RAS通路信号标志物pERK、pAKT和pS6的时间和浓度变化。结果：观察到RAS通路信号标志物pERK、pAKT和pS6的时间和浓度依赖性抑制，在Capan-2细胞中，pERK和pS6的持续抑制可达至少48小时。HPAC细胞也表现出持续的pERK抑制和时间依赖性的凋亡诱导。[2] |
| In vivo | 方法：Capan-2 (KRASG12V/WT, PDAC)和NCI-H441 (KRASG12V/WT, NSCLC)异种移植荷瘤BALB/c裸鼠用RMC-6236（3、10或25 mg/kg，口服，每天一次）治疗，在指定的时间点采集血液和肿瘤。结果：在25 mg/kg剂量下，RMC-6236能够在给药后24小时内维持超过80%的肿瘤pERK水平抑制；在10 mg/kg剂量下，RMC-6236在敏感模型中引起适度的肿瘤消退，在Capan-2和NCI-H441模型中分别导致13%和29%的平均肿瘤消退。[2] |
| Synonyms | RMC6236 |
| molecular weight | 811.05 |
| Molecular formula | C44H58N8O5S |
| CAS | 2765081-21-6 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 200 mg/mL (246.59 mM), Sonication is recommended. |
| References | 1. Ethan AHLER, et al. Use of sos1 inhibitors to treat malignancies with shp2 mutations. Patent WO2022060583A1. 2. Jiang J, et al. Translational and Therapeutic Evaluation of RAS-GTP Inhibition by RMC-6236 in RAS-Driven Cancers. Cancer Discov. 2024 Apr 9:OF1-OF24. |