计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
AKI603 is an inhibitor of Aurora kinase A (AurA) , with an IC 50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells
In Vitro
AKI603 (0.039-0.6 μM; 48 hours) extensively inhibits proliferation of leukemia cells. AKI603 (0.039-0.6 μM; 48 hours) significantly inhibits the phosphorylation of AurA in NB4, K562, and Jurkat cell lines in a dose-dependent manner while the level of total AurA protein is not changed. AKI603 inhibits the proliferation and colony formation of imatinib resistant CML cells. AKI603 (0.3-0.6 μM; 48 hours) inhibits cell proliferation and colony formation capacities in imatinib-resistant CML cells by inducing cell cycle arrest with polyploidy accumulation. Inhibition of AurA by AKI603 induces leukemia cell senescence in both BCR-ABL wild type and T315I mutation cells. AKI603 exhibits inhibitory activities on breast cancer cell proliferation, such as SUM149 (IC 50 =2.04), BT549 (IC 50 =0.86), MCF-7 (IC 50 =0.97), MCF-7-Epi (IC 50 =21.01), Sk-br-3 (IC 50 =0.73), MDA-MB-231 (IC 50 =3.49), MDA-MB-453 (MTT, IC 50 =0.18; Cell counting, IC 50 =0.19), MDA-MB-468 (MTT, IC 50 =0.15; Cell counting, IC 50 =0.17). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: U937 cells, HL-60 cells, NB4 cells, KBM5 cells, K562 cells, Jurkat cells Concentration: 0.039 μM, 0.078 μM, 0.16 μM, 0.3 μM, 0.6 μM Incubation Time: 48 hours Result: Inhibited all the tested cell lines. Western Blot AnalysisCell Line: NB4 cells, K562 cells, Jurkat cells Concentration: 0.039 μM, 0.078 μM, 0.16 μM, 0.3 μM, 0.6 μM Incubation Time: 48 hours Result: Inhibited the phosphorylation of AurA Thr288 (p-AurA). Cell Cycle AnalysisCell Line: K562, K562/G, 32D-p210 and 32D-T315I cells Concentration: 0.3 μM, 0.6 μM Incubation Time: 48 hours Result: Induced polyploidization in the tested cells.
In Vivo
AKI603 (12.5-25 mg/kg; i.p.; every 2 days; for 14 days) abrogates the growth of xenografted KBM5-T315I cells in nude mice . AKI603 exhibits moderate oral bioavailability (rat 28.7%) and C max (rat 202.4 μg/L) following oral administration (rat 25 mg/kg). AKI603 exhibits terminal elimination half-life (rat 8.9 h) following intravenous administration (rat 2.5 mg/kg). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female BALB/c nude mice, with KBM5-T315I cells xenografted Dosage: 12.5 mg/kg, 25 mg/kg Administration: Intraperitoneal injection, every 2 days, for 14 days Result: Significantly inhibited the growth of tumors. Animal Model: SD rats (220-280 g)Dosage: 2.5 mg/kg for i.v.; 25 mg/kg for p.o. (Pharmacokinetic Analysis) Administration: Intravenous injection, oral administration Result: Oral bioavailability (28.7%), C max (202.4 μg/L), T 1/2 (8.9 h)
IC50& Target:Aurora A 12.3 nM (IC 50 )
规格
规格或纯度
10mM in DMSO
英文名称
AKI603
生化机理
AKI603 是极光激酶 A（AurA）的抑制剂，IC50 为 12.3 nM。AKI603 是为克服 BCR-ABL-T315I 突变介导的耐药性而开发的。AKI603 对白血病细胞具有很强的抗增殖活性。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC1=CC(=NN1)NC2=CC(=NC(=N2)NC3=CC=C(C=C3)[N+](=O)[O-])N4CCN(CC4)C
PubChem CID
MeSH Entry Terms
AKI603
分子量
409.45
技术文档
高级数据
关联靶点（人）
AURKA
Tchem
极光激酶A(Aurora kinase A)
(1 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
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