Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Alisertib sodium (MLN 8237) is a potent and specific inhibitor (IC50 = 1.2 nM) of Aurora A kinase, an enzyme involved in cell division. By binding to Aurora A kinase, Alisertib sodium disrupts the formation of the mitotic spindle and causes abnormal cell division. At the molecular level, it acts on the AKT/mTOR/AMPK/p38 pathway, leading to the induction of apoptosis and autophagy in leukemic cells. This compound exhibits significant antitumor activity.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 13,900 | 8-10周 | ||
50 mg | ¥ 18,300 | 8-10周 | ||
100 mg | ¥ 23,500 | 8-10周 |
Alisertib sodium 的其他形式现货产品:
产品描述 | Alisertib sodium (MLN 8237) is a potent and specific inhibitor (IC50 = 1.2 nM) of Aurora A kinase, an enzyme involved in cell division. By binding to Aurora A kinase, Alisertib sodium disrupts the formation of the mitotic spindle and causes abnormal cell division. At the molecular level, it acts on the AKT/mTOR/AMPK/p38 pathway, leading to the induction of apoptosis and autophagy in leukemic cells. This compound exhibits significant antitumor activity. |
靶点活性 | Aurora A:12.5 nM (IC50), Aurora B:396.5 nM (IC50) |
体外活性 | Alisertib (MLN 8237) leads the MM cells to mitotic spindle abnormalities, mitotic accumulation, as well as inhibition of cell proliferation through apoptosis and senescence. Alisertib up-regulates p53 and tumor suppressor genes p21 and p27[1]. The decreased activity of Alisertib (MLN 8237) for the T217D/W277E Aurora A/TPX2 complex may reflect the increased affinity for ATP induced by cofactor binding to Aurora A[2]. Alisertib (MLN 8237) inhibits cell proliferation with IC 50 s ranging from 15 to 469 nM in different tumer cell lines[4]. |
体内活性 | Alisertib (MLN 8237) (30 mg/kg, p.o.) significantly reduces tumor burden and increases overall survival in xenograft-murine model of human-MM[1]. Alisertib (3-30 mg/kg; P.o.; once daily for 3 weeks) causes tumor growth inhibition in solid tumor xenograft models[4]. Animal Model: Nude mice bearing HCT-116 colon tumor xenograft[4]Dosage: 3, 10, or 30 mg/kg Administration: P.o.; once daily for 3 weeks Result: Resulted in a dose-dependent TGI (tumor growth inhibition) of 43.3%, 84.2%, and 94.7% for the 3, 10, and 30 mg/kg groups,respectively. |
别名 | MLN 8237 sodium |
分子量 | 541.92 |
分子式 | C27H20ClFN4NaO4 |
CAS No. | 1028486-06-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Alisertib sodium 1028486-06-7 MLN 8237 sodium Inhibitor inhibitor inhibit