SOP1812 (QN-302) 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 K D values of 4.9 and 28.4 nM, respectively. SOP1812 can be used for the research of cancer.
In Vitro
SOP1812 (0-50 nM; 96 h) inhibits the proliferation of many cancer cells. SOP1812 (0-800 nM; 6-24 h) shows great affinity to hTERT G4 and HuTel21 G4. SOP1812 (40 nM; 6-24 h) affects Wnt/β-catenin, axon guidance, Hippo, MAPK and Rap1 pathways. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell 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 GI 50 values of 1.3, 1.4, 5.9 and 2.6 nM, respectively. Cell Viability AssayCell 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 K D values of 4.9 and 28.4 nM, respectively. Cell Viability AssayCell 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.
In Vivo
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female athymic nude mice with MIA PaCa-2 xenografts 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 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.
Form:Solid
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| Solubilità | DMSO : 200 mg/mL (252.53 mM; Need ultrasonic) |
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