Bioactivity | PRO-6E is an oral active PROTAC based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells. PRO-6E inhibits tumor growth in vivo and in vitro. PRO-6E induces cell apoptosis and induces cell arrest (Sturcture Note:(Blue: Cereblon ligand (HY-103596), Black: linker;Pink: ALK/c-Met inhibitor Crizotinib (HY-50878))[1]. | ||||||||||||
Invitro | PRO-6E (0.03-10 μM; 48 h) 对 MKN-45、SNU-638 细胞生长的抑制作用[1]。PRO-6E (1 μM; 超过24 h) 促进 MKN-45 细胞 MET 降解[1]。PRO-6E (0.1-1 μM; 48 h) 使 MKN-45 细胞中 G2/M 相细胞百分比增加,S 相细胞百分比减少[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PRO-6E 相关抗体: Cell Viability Assay[1] Cell Line: | ||||||||||||
In Vivo | PRO-6E (口服; 30 mg/kg/天; 持续15天) 抑制 MKN - 45 细胞来源的异种移植肿瘤模型的肿瘤生长[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: | ||||||||||||
CAS | 2353493-69-1 | ||||||||||||
Formula | C42H44Cl2FN7O7 | ||||||||||||
Molar Mass | 848.75 | ||||||||||||
Appearance | 固体 | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Chen JJ, et al. Crizotinib-based proteolysis targeting chimera suppresses gastric cancer by promoting MET degradation. Cancer Sci. 2023;114(5):1958-1971. |