SOP1812 is a naphthalene diimide (ND) derivative with anti-tumor activity. SOP1812 binds to quadruplex arrangements (G4s), and down-regulates several cancer gene pathways. SOP1812 shows great affinity to hTERT G4 and HuTel21 G4 with KD values of 4.9 and 28.4 nM, respectively. SOP1812 can be used for the research of cancer[1].
SOP1812 (0-50 nM; 96 h) inhibits the proliferation of many cancer cells[1].
SOP1812 (0-800 nM; 6-24 h) shows great affinity to hTERT G4 and HuTel21 G4[1].
SOP1812 (40 nM; 6-24 h) affects Wnt/β-catenin, axon guidance, Hippo, MAPK and Rap1 pathways[1].
Cell Proliferation Assay[1]
| Cell Line: | MIA PaCa-2, PANC-1, Capan-1 and BxPC-3 cell lines |
| Concentration: | 0-50 nM |
| Incubation Time: | 96 hours |
| Result: | Showed anti-proliferation ability to MIA PaCa-2, PANC-1, Capan-1 and BxPC-3 cells with GI50 values of 1.3, 1.4, 5.9 and 2.6 nM, respectively. |
Cell Viability Assay[1]
| Cell Line: | PANC-1 cells |
| Concentration: | 0, 100, 400 and 800 nM |
| Incubation Time: | 6 and 24 hours |
| Result: | Binded to hTERT G4 and HuTel21 G4 with KD values of 4.9 and 28.4 nM, respectively. |
Cell Viability Assay[1]
| Cell Line: | MIA PaCa-2 Cells |
| Concentration: | 40 nM |
| Incubation Time: | 6 and 24 hours |
| Result: | Affected WNT5B, DVL1, AXIN and APC2 expression which includes in Wnt/β-catenin pathway and also showed effects on axon guidance, Hippo, MAPK, and Rap1 pathways. |
SOP1812 (1 mg/kg; i.v. once or twice per week for 28 days) shows anti-tumor activity in MIA PaCa-2 xenografts mice and KPC mice[1].
| Animal Model: | Female athymic nude mice with MIA PaCa-2 xenografts[1] |
| Dosage: | 1 mg/kg |
| Administration: | Intravenous injection; 1 mg/kg once or twice per week; for 28 days |
| Result: | Showed complete tumor regression and no significant tumor regrowth after day 28 on several animals. |
| Animal Model: | KPC mice with PDAC symptoms[1] |
| Dosage: | 1 mg/kg |
| Administration: | Intravenous injection; 1 mg/kg once per week; for 3 weeks |
| Result: | Significantly extended survival of KPC mice and showed a better effect than gemcitabine. |