| Identification | Back Directory | [Name]
Evo312 | [CAS]
2820245-53-0 | [Synonyms]
Evo312
Indolo[2′,3′:3,4]pyrido[2,1-b]quinazolin-5(7H)-one, 10-(acetyloxy)-8,13,13b,14-tetrahydro-14-methyl- | [Molecular Formula]
C21H19N3O3 | [MOL File]
2820245-53-0.mol | [Molecular Weight]
361.39 |
| Chemical Properties | Back Directory | [Boiling point ]
627.964±55.00 °C(Press: 760.00 Torr)(predicted) | [density ]
1.433±0.10 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | [pka]
16.626±0.20(predicted) |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
Evo312 (5 mg/kg, ip., three times a week, 20 days) inhibits tumor growth in the PANC-GR (Gemcitabine-resistant cells) mouse xenograft model by inhibiting PKCβⅠ, whereas gemcitabine treatment resulted in negligible inhibitory effects on tumor growth[1]. | Animal Model: | PANC-GR cell mouse xenograft model; PANC-1 cell mouse xenograft model[1] | | Dosage: | 40 mg/kg; 5 mg/kg, three times a week, 20 days | | Administration: | Intraperitoneal injection (i.p.) | | Result: | Did not cause mouse death or significant toxicity at a dose of 40 mg/kg. At a dose of 5 mg/kg, the tumor volume was inhibited by 72%, and the tumor weight was reduced by 44.89% compared with the drug-loaded treatment group, with no significant toxicity or weight changes, and the expression of PKCβI in tumor tissues implanted with PANC-GR cells was effectively inhibited. |
| [IC 50]
PKC-βI: 117.34 nM (IC50) | [References]
[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. DOI:10.1021/acs.jmedchem.4c00213 |
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