| Bioactivity | Evo312 is a dose-dependent inhibitor of protein kinase CβⅠ (PKCβⅠ) (IC50 is 117.34 nM). Evo312 induces PANC-GR (acquired gemcitabine-resistant PC cells) cell cycle arrest and apoptosis by inhibiting PKCβ1 protein expression. Evo312 has antiproliferative effects in pancreatic cancer cells PANC-1 and PANC-GR cells with IC50 of 0.08 μM and 0.07 μM, and in human normal pancreatic ductal epithelial cells HPDE6-c7 with IC50 of 2.95 μM. Evo312 exhibits antitumor activity in a PANC-GR cell transplantation mouse model[1]. |
| Invitro | Evo312 (0-160 nM，24 h) 抑制 PANC-GR 细胞中 PKCβ1 蛋白表达和下游靶蛋白磷酸化[1]。Evo312 (0-160 nM，24 h) 诱导 PANC-GR 细胞 G2/M 细胞周期阻滞，抑制细胞有丝分裂[1]。Evo312 (0-160 nM，48 h) 诱导 PANC-GR 细胞凋亡[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Evo312 相关抗体: Cell Cycle Analysis[1] Cell Line: |
| In Vivo | Evo312 (5 mg/kg，i.p.，three times a week，20 days) 通过下调 PKCβⅠ 抑制 PANC-GR (吉西他滨耐性细胞) 小鼠异种移植模型的肿瘤生长，而吉西他滨治疗对肿瘤生长的抑制作用可以忽略不计[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 2820245-53-0 |
| Formula | C21H19N3O3 |
| Molar Mass | 361.39 |
| 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]. Eun Seo Bae, et al. Evo312: An Evodiamine Analog and Novel PKCβI Inhibitor with Potent Antitumor Activity in Gemcitabine-Resistant Pancreatic Cancer. J Med Chem. 2024 Aug 16. |