SOP1812

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].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> G-quadruplex

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.

[1]. Ahmed AA, et al. Asymmetrically Substituted Quadruplex-Binding Naphthalene Diimide Showing Potent Activity in Pancreatic Cancer Models. ACS Med Chem Lett. 2020 Jul 16;11(8):1634-1644.