Bioactivity | 3-Fluoro-evodiamine glucose (Compound 8) is an evodiamine-glucose conjugate. 3-Fluoro-evodiamine glucose activates the expression of glucose transporter 1 (GLUT1), and inhibits topoisomerase I/II. 3-Fluoro-evodiamine glucose induces apoptosis and arrests the cell cycle at G2/M phase. 3-Fluoro-evodiamine glucose exhibits antitumor efficacy in vivo and in vitro, without significant toxicity[1]. |
Invitro | 3-Fluoro-evodiamine glucose (0-0.5 μM,12 h) 通过诱导活性氧 (ROS) 积累和 DNA 损伤,在癌细胞 U87MG、A549 和 HCT116 中表现出抗增殖活性和细胞毒性,IC50 为 0.064–0.113 μM[1]。3-Fluoro-evodiamine glucose (0-0.05 μM,24 h) 剂量依赖地抑制 HCT116 细胞的迁移和侵袭[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> 3-Fluoro-evodiamine glucose 相关抗体: Western Blot Analysis[1] Cell Line: |
In Vivo | 3-Fluoro-evodiamine glucose (10 mg/kg,腹腔注射,单剂量) 在小鼠体内表现出良好的药代动力学特性,半衰期为 2.41 h,血浆暴露度 Cmax 为 4627 h·ng/ mL,AUC0-t 为 4008 h·ng/mL,平均停留时间为 0.802 h[1]。3-Fluoro-evodiamine glucose (10-20 mg/kg,腹腔注射,每天两次,持续 21 天) 在 HCT116 异种移植裸鼠中表现出抗肿瘤功效,肿瘤生长抑制率 TGI 为 72%-82%,且无明显毒性[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
Formula | C25H26FN3O7 |
Molar Mass | 499.49 |
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]. Wu Z, et al., Design of Evodiamine-Glucose Conjugates with Improved In Vivo Antitumor Activity. J Med Chem. 2024 May 9;67(9):7373-7384. |