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。
| 生物活性 | SOP1812 is a naphthalene diimide (ND) derivative with anti-tumor activity. SOP1812 binds toquadruplex arrangements (G4s), and down-regulates severalcancergene 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 ofcancer[1]. |
体外研究
(In Vitro) | 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. |
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体内研究
(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[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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 200 mg/mL(252.53 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.2627 mL | 6.3133 mL | 12.6266 mL | | 5 mM | 0.2525 mL | 1.2627 mL | 2.5253 mL | | 10 mM | 0.1263 mL | 0.6313 mL | 1.2627 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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