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SOP1812

カタログ番号GC65887

SOP1812 は、抗腫瘍活性を持つナフタレンジイミド (ND) 誘導体です。 SOP1812 は四重鎖配置 (G4) に結合し、いくつかの癌遺伝子経路をダウンレギュレートします。 SOP1812 は、hTERT G4 および HuTel21 G4 に対して高い親和性を示し、KD 値はそれぞれ 4.9 および 28.4 nM です。 SOP1812 は、がんの研究に使用できます。

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SOP1812 化学構造

Cas No.: 2546091-70-5

サイズ 価格 在庫数 個数
10mg
$765.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents

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.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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