Bioactivity | Anticancer agent 114 is a potent and orally active dipeptide boronic acid ester proteasome inhibitor with an IC50 value of 2.2 nM. Anticancer agent 114 has antiproliferative activity against the RPMI-8226 cells. Anticancer agent 114 can be used in research of multiple myeloma[1]. |
Invitro | Anticancer agent 114 (compound 18u; 0-2 μM; 24 h) 对 RPMI-8226 细胞具有抗增殖活性,IC50 值为 5.6 nM[1]。 Cell Viability Assay[1] Cell Line: |
In Vivo | Anticancer agent 114 (compound 18u; 6 and 10 mg/kg; p.o.; 每周两次, 持续 21 天) 在人 MM (RPMI-8226) 异种移植小鼠模型中表现出抗癌功效[1]。Anticancer agent 114 (0.4 mg/kg and 1.2 mg/kg; i.v and p.o.; 雄性 Sprague-Dawley 大鼠) 表现出良好的微粒体稳定性和药代动力学特性[1]。 Animal Model: |
Name | Anticancer agent 114 |
Formula | C28H33BF6N2O7 |
Molar Mass | 634.37 |
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]. Wang X, et, al. Design and discovery of novel dipeptide boronic acid ester proteasome inhibitors, an oral slowly-released prodrug for the treatment of multiple myeloma. Eur J Med Chem. 2023 Mar 15;250:115187. |