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抑制剂/激活剂

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凋亡与自噬

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Alisertib MLN 8237

Alisertib (MLN8237)是一种选择性Aurora A抑制剂，无细胞试验中IC50为1.2 nM，作用于Aurora A比作用于Aurora B选择性强200倍以上。Alisertib 可诱导细胞周期阻滞、细胞凋亡与自噬。Phase 3。

货号：
TK0143
规格：

1mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	1028486-01-2
生物活性	Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.
分子式	C27H20ClFN4O4
分子量	518.92
储存条件	Powder -20℃ 3 years
溶解性数据	DMSO : 25 mg/mL (48.18 mM; Need ultrasonic)
体内研究	Alisertib (MLN 8237) (30 mg/kg, p.o.) significantly reduces tumor burden and increases overall survival in xenograft-murine model of human-MM. Alisertib (3-30 mg/kg; p.o.; once daily for 3 weeks) causes tumor growth inhibition in solid tumor xenograft models.
体外研究	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. 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. Alisertib (MLN 8237) inhibits cell proliferation with IC50s ranging from 15 to 469 nM in different tumer cell lines.
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纯度及产品资料	98%

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