SOP1812
目录号 : GC65887
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
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. |
| Cas No. | 2546091-70-5 | SDF | Download SDF |
| 分子式 | C45H57N7O6 | 分子量 | 791.98 |
| 溶解度 | 储存条件 | Store at -20°C | |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Asymmetrically Substituted Quadruplex-Binding Naphthalene Diimide Showing Potent Activity in Pancreatic Cancer Models
ACS Med Chem Lett 2020 Jul 16;11(8):1634-1644.PMID:32832034DOI:PMC7429975
Targeting of genomic quadruplexes is an approach to treating complex human cancers. We describe a series of tetra-substituted naphthalene diimide (ND) derivatives with a phenyl substituent directly attached to the ND core. The lead compound (SOP1812) has 10 times superior cellular and in vivo activity compared with previous ND compounds and nanomolar binding to human quadruplexes. The pharmacological properties of SOP1812 indicate good bioavailability, which is consistent with the in vivo activity in xenograft and genetic models for pancreatic cancer. Transcriptome analysis shows that it down-regulates several cancer gene pathways, including Wnt/β-catenin signaling.