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10074-G5是一种c-Myc-Max 二聚化的抑制剂,IC50值为146 μM。
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10074-G5是一种c-Myc-Max 二聚化的抑制剂,IC50值为146 μM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
2 mg | ¥ 283 | 现货 | |
5 mg | ¥ 497 | 现货 | |
10 mg | ¥ 690 | 现货 | |
25 mg | ¥ 1,150 | 现货 | |
50 mg | ¥ 1,930 | 现货 | |
100 mg | ¥ 3,360 | 现货 | |
200 mg | ¥ 4,890 | 现货 | |
500 mg | ¥ 7,580 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 547 | 现货 |
产品描述 | 10074-G5 is an inhibitor of c-Myc-Max dimerization. |
靶点活性 | c-Myc:2.8 μM(Kd) |
体外活性 | 10074-G5通过结合并扭曲c-Myc的bHLH-ZIP结构域,从而抑制c-Myc/Max异源二聚体的形成以及其转录活性。在体外实验中,10074-G5能够抑制Daudi Burkitt's淋巴瘤细胞的生长,并且破坏c-Myc/Max二聚体的形成。Daudi细胞积累10074-G5,且最高的细胞内浓度在6小时时观察到。在Daudi细胞中,10074-G5能够在4小时时约75%地抑制c-Myc/Max二聚体的形成,这种抑制作用在24小时的培养时间内得以维持。c-Myc的总蛋白表达也相应减少,经10 μM 10074-G5处理24小时后,c-Myc蛋白表达量与对照组相比约减少了40%。在体外,10074-G5对过表达c-Myc的Daudi和HL-60细胞具有细胞毒性[2]。 |
体内活性 | 在小鼠体内,通过静脉注射20 mg/kg 10074-G5后,其血浆半衰期为37分钟,峰值血浆浓度达到58 μM,这是峰值肿瘤浓度的10倍。10074-G5的抗肿瘤活性不足可能由其快速代谢成无活性代谢物导致,从而使得肿瘤中10074-G5的浓度不足以抑制c-Myc/Max二聚体形成。在给予小鼠携带Daudi异种移植瘤20 mg/kg 10074-G5的静脉注射后5分钟,观察到58.5 ± 2.7 nmol/ml的10074-G5血浆峰值浓度(Cmax),此后10074-G5在血浆中的浓度迅速下降。除了在肺、肝和脂肪中,10074-G5在所有时间点的组织浓度均低于血浆浓度[2]。 |
细胞实验 | Daudi cells (3 × 108 cells in logarithmic growth) are incubated for 0, 1, 3, 6, or 24 h in 3 ml of complete medium containing 10 μM 10074-G5. After incubation, cells are harvested, split into two samples of 1.5 ml each, and overlaid in microcentrifuge tubes containing 0.5 ml of silicon oil. The tubes are centrifuged at 12,000 g for 4 min. After centrifugation, the top 1 ml of medium is removed and stored in cryovials at ?70°C until analysis. The remaining medium and silicon oil are carefully removed without disturbing the cell pellets. The sides of the tubes are cleaned with cotton-tipped applicators, and the cell pellets are stored at ?70°C until analysis.(Only for Reference) |
分子量 | 332.31 |
分子式 | C18H12N4O3 |
CAS No. | 413611-93-5 |
Smiles | [O-][N+](=O)c1ccc(Nc2ccccc2-c2ccccc2)c2nonc12 |
密度 | 1.408 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 55 mg/mL (165.51 mM), Sonication is recommended. Ethanol: 10 mg/mL (30.09 mM) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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