SOP1812 是一种 naphthalene diimide (ND) 衍生物，具有抗肿瘤活性。SOP1812 能够与quadruplex arrangements (G4s) 结合，并下调多个癌症基因通路。SOP1812 对 hTERT G4 和 HuTel21 具有很强的亲和力，其 KD 值分别为 4.9 和 28.4 nM。G4SOP1812 可用于癌症的研究。
| Cas No. | 2546091-70-5 |
| 分子式 | C45H57N7O6 |
| 分子量 | 791.98 |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | SOP1812 is a naphthalene diimide (ND) derivative with anti-tumor activity. SOP1812 binds toquadruplex arrangements (G4s), and down-regulates several cancer gene pathways. SOP1812 shows great affinity to hTERT G4 and HuTel21 G4 withKDvalues 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 GI50values 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 withKDvalues 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. |
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