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Alisertib {[allProObj[0].p_purity_real_show]}

货号：A102516 同义名： MLN 8237

Alisertib (MLN 8237) 是一种口服活性和选择性的 Aurora A 激酶抑制剂 (IC50 = 1.2 nM)，通过结合 Aurora A 激酶引起纺锤体异常和有丝分裂积累。Alisertib (MLN 8237) 通过靶向 AKT/mTOR/AMPK/p38 通路在白血病细胞中诱导凋亡和自噬，显示出抗肿瘤活性。

Alisertib 化学结构 CAS号：1028486-01-2
Alisertib 化学结构
CAS号：1028486-01-2
Alisertib 3D分子结构
CAS号：1028486-01-2
Alisertib 化学结构 CAS号：1028486-01-2
Alisertib 3D分子结构 CAS号：1028486-01-2
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Alisertib 纯度/质量文件 产品仅供科研

货号：A102516 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Aurora A ↓ Aurora B ↓ Aurora C ↓ 其他靶点 纯度
BI-847325 ++

Aurora A (Human), IC50: 25 nM

 		++++

Aurora B (Xenopus laevis), IC50: 3 nM

 		++

Aurora C (Human), IC50: 15 nM

 		99%+
CCT 137690 ++

Aurora A, IC50: 15 nM

 		++

Aurora B, IC50: 25 nM

 		++

Aurora C, IC50: 19 nM

 		99%+
MK-5108 ++++

Aurora A, IC50: 0.064 nM

 		99%+
KW-2449 +

Aurora A, IC50: 48 nM

 		FLT3 99%+
Tozasertib ++++

Aurora A, Ki app: 0.6 nM

 		++

Aurora B, Ki app: 18 nM

 		+++

Aurora C, Ki app: 4.6 nM

 		Bcr-Abl,FLT3 99%+
AT9283 ++++

Aurora A, IC50: ~3.0 nM

 		++++

Aurora B, IC50: ~3.0 nM

 		99%+
MLN8054 +++

Aurora A, IC50: 4 nM

 		+

Aurora B, IC50: 172 nM

 		99%+
ZM-447439 +

Aurora A, IC50: 110 nM

 		+

Aurora B, IC50: 130 nM

 		Src 99%+
TCS7010 ++++

Aurora A, IC50: 3.4 nM

 		99%+
TAK-901 ++

Aurora A-TPX2, IC50: 21 nM

 		++

Aurora B-INCENP, IC50: 15 nM

 		99%+
Danusertib +++

Aurora A, IC50: 13 nM

 		+

Aurora B, IC50: 79 nM

 		+

Aurora C, IC50: 61 nM

 		RET 99%+
MK-8745 ++++

Aurora A, IC50: 0.6 nM

 		99+%
PHA-680632 ++

Aurora A, IC50: 27 nM

 		+

Aurora B, IC50: 135 nM

 		+

Aurora C, IC50: 120 nM

 		FLT3 99%+
AMG 900 +++

Aurora A, IC50: 5 nM

 		+++

Aurora B, IC50: 4 nM

 		++++

Aurora C, IC50: 1 nM

 		99%+
Alisertib ++++

Aurora A, IC50: 1.2 nM

 		99%+
ENMD-2076 +++

Aurora A, IC50: 14 nM

 		+

Aurora B, IC50: 350 nM

 		FLT3,RET 98%
JNJ-7706621 +++

Aurora A, IC50: 11 nM

 		++

Aurora B, IC50: 15 nM

 		99%+
CYC-116 +++

Aurora A, Ki: 8 nM

 		+++

Aurora B, Ki: 9 nM

 		FLT3 99%+
Reversine +++

Aurora A, IC50: 12 nM

 		+++

Aurora B, IC50: 13 nM

 		++

Aurora C, IC50: 20 nM

 		98%
CCT129202 ++

Aurora A, IC50: 42 nM

 		+

Aurora B, IC50: 198 nM

 		+

Aurora C, IC50: 227 nM

 		98%
SNS-314 mesylate +++

Aurora A, IC50: 9 nM

 		++

Aurora B, IC50: 31 nM

 		++++

Aurora C, IC50: 3 nM

 		99%+
Barasertib-HQPA ++++

Aurora B, IC50: 0.37 nM

 		99%+
Hesperadin +

Aurora B (human), IC50: 250 nM

 		98%
GSK-1070916 ++++

Aurora B-INCENP, IC50: 3.5 nM

 		+++

Aurora C-INCENP, IC50: 6.5 nM

 		SIK,Tie-2 99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Alisertib 生物活性

靶点

  • Aurora A

    Aurora A, IC50:1.2 nM
描述 The Aurora family of serine/threonine kinases, which consists of Aurora A, B and C, plays an important role in chromosome alignment, segregation, and cytokinesis during mitosis. Alisertib is a selective Aurora A kinase inhibitor with IC50 value of 1.2nM versus 396.5nM for Aurora B (measured by enzymatic assay). Consistent with inhibition by Aurora A on cell phenotype, treatment with 50nM Alisertib casued an increase in cells in the G2/M phase at 24 and 48 hours in HCT-116 cells, as well as caused mitotic spindle abnormalities and chromosome misalignment in cells. However, at a higher concentration of 0.25 or 1μM, Alisertib caused an increase in the number of cells with 8N DNA content and multinuclear in cells, as phenotypes consistent with Aurora B inhibition. Alisertib can inhibit cell proliferation, including HCT-116, SW480, DLD-1, H460, MDA-MB-231, PC3, SKOV3, HPAC, OCI-LY-3, OCI-LY-7, OCI-LY-10, OCI-LY-19 and WSU cell lines, with IC50 values ranging in 15-469nM, suggesting its widely anti-proliferative effect on colon, lung, breast, prostate, ovarian, pancreatic and lymphoma tumor. Alisertib possessed good pharmacodynamics as orally dosed at 3, 10, and 30mg/kg with Alisertib resulted in a time- and dose-dependent increase in the mitotic marker p-HisH3, suggesting Aurora A inhibition, in tumor tissue from HCT-116 xenografts. Misaligned chromosomes and reduced bipolar mitotic spindles can also be observed. Oral administration of Alisertib at 3, 10, and 30 mg/kg once daily for 21 consecutive days dose-dependently inhibit tumor growth in nude mice bearing subcutaneous HCT-116 tumors. The broad antitumor activity of Alisertib can also be observed in a diverse set of solid tumor xenograft models as well as regressions in in vivo models of lymphoma, including the cell lines mentioned above[1].
作用机制 Alisertib binds Aurora-A at the ATP-binding pocket.[2]

Alisertib 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
2884 100 μM Growth Inhibition Assay 72 h Attenuates cell growth 23328114
2885 100 μM Growth Inhibition Assay 72 h Attenuates cell growth 23328114
A172 100 μM Cytotoxic Assay 24 h IC50=0.120 μM 22274399
A-673 10 μM Growth Inhibition Assay 96 h IC50=0.032 μM 21448591

Alisertib 动物研究

Dose Mice: min = 3mg/kg, max =30 mg/kg[1]
Administration p.o.

Alisertib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02551055 Neoplasms, Advanced or Metasta... 展开 >>tic 收起 << Phase 1 Terminated(Business Decision; ... 展开 >>No Safety Or Efficacy Concerns.) 收起 << - United States, New York ... 展开 >> Lake Success, New York, United States New York, New York, United States United States, Pennsylvania Philadelphia, Pennsylvania, United States United States, Texas Dallas, Texas, United States Houston, Texas, United States Spain Barcelona, Spain 收起 <<
NCT01540682 Head and Neck Cancer Phase 1 Completed - United States, Pennsylvania ... 展开 >> Abramson Cancer Center of the University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 收起 <<
NCT01316692 Recurrent Melanoma ... 展开 >> Stage IIIc Melanoma Stage IV Melanoma 收起 << Phase 2 Terminated(low accrual) - United States, Tennessee ... 展开 >> Vanderbilt-Ingram Cancer Center Nashville, Tennessee, United States, 37232-6838 收起 <<

Alisertib 参考文献

[1]Manfredi MG, Ecsedy JA, et al. Characterization of Alisertib (MLN8237), an investigational small-molecule inhibitor of aurora A kinase using novel in vivo pharmacodynamic assays. Clin Cancer Res. 2011;17(24):7614-24.

[2]Asteriti IA, Daidone F, et al. Identification of small molecule inhibitors of the Aurora-A/TPX2 complex. Oncotarget. 2017;8(19):32117-32133.

Alisertib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.93mL

0.39mL

0.19mL

9.64mL

1.93mL

0.96mL

19.27mL

3.85mL

1.93mL

Alisertib 技术信息

CAS号1028486-01-2
分子式C27H20ClFN4O4
分子量 518.923
别名 MLN 8237
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Inert atmosphere,2-8°C
溶解度

DMSO: 25 mg/mL(48.18 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 1.6 mg/mL clear

PO 0.5% CMC-Na 36 mg/mL suspension

Tags: Alisertib | 1028486-01-2 | MLN 8237 | MLN8237 | MLN-8237 | Aurora A Kinase Inhibitor | Cell Cycle/DNA Damage | Epigenetics | Autophagy | Apoptosis | Aurora Kinase | Autophagy | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Alisertib 纯度/质量文件 | Alisertib 亚型比较 | Alisertib 生物活性 | Alisertib 细胞研究 | Alisertib 动物研究 | Alisertib 临床数据 | Alisertib 参考文献 | Alisertib 实验方案 | Alisertib 技术信息

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