2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. Aurora Kinase HDAC Apoptosis
  4. Aurora kinase/HDAC-IN-1

Aurora kinase/HDAC-IN-1 是一种口服有效的的 Aurora 激酶与 HDAC 双靶点抑制剂，可抑制 Aurora A (IC50 = 116 nM)、Aurora B (IC50 = 225 nM)、HDAC1 (IC50 = 164 nM)和 HDAC2 (IC50 = 346 nM)。Aurora kinase/HDAC-IN-1 可促进组蛋白乙酰化 (Ac-H3) ，抑制 Aurora A 磷酸化及其下游信号，并通过 G2/M 期阻滞诱导细胞凋亡 (apoptosis)。Aurora kinase/HDAC-IN-1 在结直肠癌细胞 HCT-116 中表现出显著的抗增殖活性，IC50 为 30.2 nM。Aurora kinase/HDAC-IN-1 可在 HCT-116 结直肠癌异种移植小鼠模型中显著抑制肿瘤生长。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

Aurora kinase/HDAC-IN-1

Aurora kinase/HDAC-IN-1 Chemical Structure

CAS No. : 2727102-12-5

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

Aurora kinase/HDAC-IN-1 相关抗体

Top Publications Citing Use of Products

查看 Aurora Kinase 亚型特异性产品:

查看所有亚型
Aurora Kinase Aurora A Aurora B Aurora C

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Aurora kinase/HDAC-IN-1 is an orally active dual Aurora kinase and HDAC inhibitor that inhibits Aurora A (IC50 = 116 nM), Aurora B (IC50 = 225 nM), HDAC1 (IC50 = 164 nM), and HDAC2 (IC50 = 346 nM).Aurora kinase/HDAC-IN-1 promotes histone H3 acetylation, inhibits Aurora A phosphorylation and downstream signaling, and induces apoptosis via G2/M cell-cycle arrest. Aurora kinase/HDAC-IN-1 exhibits potent antiproliferative activity in colorectal cancer cells, with an IC50 value of 30.2 nM in HCT-116 cells.Aurora kinase/HDAC-IN-1 significantly suppresses tumor growth in an HCT-116 colorectal cancer xenograft mouse model[1].

IC50 & Target[1]

Aurora A

116 nM (IC50)

Aurora B

225 nM (IC50)

HDAC1

164 nM (IC50)

HDAC2

346 nM (IC50)

体外研究
(In Vitro)

Aurora kinase/HDAC-IN-1 (compound 6) (0.64 nM-10 μM；72 小时) 可抑制 HCT-116 与 MIA PaCa-2 细胞增殖，IC50 分别为 30.2 nM 和 42.8 nM[1]。
Aurora kinase/HDAC-IN-1 (30-120 nM;24 小时) 可在 HCT-116 细胞中诱导 G2/M 期阻滞[1]。
Aurora kinase/HDAC-IN-1 (30-120 nM;48 小时) 可在 HCT-116 细胞中诱导细胞凋亡[1]。
Aurora kinase/HDAC-IN-1 (30-120 nM;72 小时) 可调控 HCT-116 细胞中 Aurora/HDAC 相关信号，包括促进 Ac-H3 并抑制 Aurora A 磷酸化[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Aurora kinase/HDAC-IN-1 相关抗体:

Cell Viability Assay[1]

Cell Line: HCT-116 cells; MIA PaCa-2 cells
Concentration: 0.64 nM-10 μM
Incubation Time: 72 h
Result: Inhibited HCT-116 cell proliferation with an IC50 value of 30.2 nM.
Inhibited MIA PaCa-2 cell proliferation with an IC50 value of 42.8 nM.

Cell Cycle Analysis[1]

Cell Line: HCT-116 cells
Concentration: 30 nM, 60 nM, 120 nM
Incubation Time: 24 h
Result: Increased G2/M-phase population from 5.03% (control) to 12.68% (30 nM), 20.17% (60 nM), and 25.40% (120 nM).

Apoptosis Analysis[1]

Cell Line: HCT-116 cells
Concentration: 30 nM, 60 nM, 120 nM
Incubation Time: 48 h
Result: Increased apoptosis rate from 1.99% (control) to 21.03% (30 nM), 42.81% (60 nM), and 59.13% (120 nM).

Western Blot Analysis[1]

Cell Line: HCT-116 cells
Concentration: 30 nM, 60 nM, 120 nM
Incubation Time: 72 h
Result: Increased Ac-H3 expression and upregulated p53 and Caspase 3 expression, and reduced p-Aurora A levels.
体内研究
(In Vivo)

Aurora kinase/HDAC-IN-1 (compound 6) (50-150 mg/kg/d; 口服 p.o.; 每日一次 QD; 连续 21 天) 可在 HCT-116 结直肠癌异种移植小鼠模型中显著抑制肿瘤生长 (150 mg/kg/d 时 TGI = 71.8%)，并在小鼠中表现出较好的口服生物利用度 (F = 23.2%)[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c nude mice (6-8 weeks old) bearing subcutaneous HCT-116 xenografts [1]
Dosage: 50 mg/kg/d, 150 mg/kg/d
Administration: Oral gavage (p.o.), once daily (QD), for 21 days.
Result: Inhibited tumor growth in HCT-116 colorectal cancer xenograft mice, resulting in a significant reduction in tumor volume without obvious toxicity.
Increased tumor necrosis and reduced Ki67 staining (decreased proliferation), with more pronounced effects at 150 mg/kg/d.
分子量

449.50

Formula

C22H20FN7OS
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Aurora kinase/HDAC-IN-1 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Aurora kinase/HDAC-IN-12727102-12-5Aurora KinaseHDACApoptosisHistone deacetylasesAurora AAurora B,HDACdual inhibitorcolorectal cancerHCT-116 cellsxenograft modelInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
Aurora kinase/HDAC-IN-1
目录号：
HY-179374
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z