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Vinblastine 抑制微管形成并抑制 nAChR 活性,IC50 为 8.9 μM,用于治疗某些类型的癌症。
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Vinblastine 抑制微管形成并抑制 nAChR 活性,IC50 为 8.9 μM,用于治疗某些类型的癌症。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥ 391 | 5日内发货 | |
10 mg | ¥ 705 | 5日内发货 | |
25 mg | ¥ 1,268 | 5日内发货 | |
50 mg | ¥ 2,294 | 5日内发货 | |
100 mg | ¥ 3,620 | 5日内发货 | |
200 mg | ¥ 6,516 | 5日内发货 | |
1 mL x 10 mM (in DMSO) | ¥ 705 | 5日内发货 |
产品描述 | Vinblastine inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM, used to treat certain kinds of cancer. |
靶点活性 | nAChR:8.9 μM |
体外活性 | Vinblastine does not depolymerize spindle microtubules, yet it powerfully blocks mitosis (for example, IC50 0.8 nM in HeLa cells) and cells die by apoptosis[2]. In NB4 cells, vinblastine produces alteration of p53 and DNA fragmentation. Vinblastine treatment has an antiproliferative effect via the induction of apoptosis producing Bax/Bcl-2 imbalance. Vinblastine treatment suppresses NFκB expression and depresses NFκB-DNA binding activity while maintaining JNK activation that subsequently results in apoptotic response through caspase-dependent pathway[3]. Vinblastine is found to trigger apoptosis as evidenced by the loss of mitochondrial membrane potential, the release of both cytochrome c and apoptosis inducing factor, activation of caspase-9 and 3, and cleavage of Poly (ADP-ribose)-Polymerase[4]. |
体内活性 | Vinblastine is a widely used anticancer drug with undesired side effects. Its conjugation with carrier molecules could be an efficient strategy to reduce these side effects[5]. |
细胞实验 | Six-well treatment plates are set up that contained 5 × 104 cells/mL in each well, suspended in 3 mL culture medium, and these are treated with vinblastine for 3 h followed by 21 h growth. (Only for Reference) |
别名 | 长春质碱 |
分子量 | 810.97 |
分子式 | C46H58N4O9 |
CAS No. | 865-21-4 |
密度 | 1.37 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||
溶解度信息 | Ethanol: 6 mg/mL (7.39 mM) DMSO: 42 mg/mL | |||||||||||||||
溶液配制表 | ||||||||||||||||
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