2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. Tubulin polymerization-IN-92

Tubulin polymerization-IN-92，KX-01 (HY-10340) 的类似物，是一种强效口服活性微管蛋白聚合 (tubulin polymerization) 抑制剂，其与微管蛋白结合的 Ka 值为 1.29 μM。Tubulin polymerization-IN-92 可同时占据 β-微管蛋白中的秋水仙碱结合位点以及 α-微管蛋白中的一个空腔。Tubulin polymerization-IN-92 具有抗增殖活性，可诱导癌细胞发生 G2/M 期细胞周期阻滞和凋亡 (apoptosis)。Tubulin polymerization-IN-92 可抑制小鼠异种移植模型中的肿瘤生长。Tubulin polymerization-IN-92 可用于结肠癌、宫颈癌以及紫杉醇 (HY-B0015) 耐药性卵巢癌的研究。

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

Tubulin polymerization-IN-92

Tubulin polymerization-IN-92 Chemical Structure

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

Tubulin polymerization-IN-92 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tubulin polymerization-IN-92, an analog of KX-01 (HY-10340), is a potent orally active tubulin polymerization inhibitor that binds tubulin with a Ka of 1.29 μM. Tubulin polymerization-IN-92 simultaneously occupies the colchicine site in β-tubulin and a cavity in α-tubulin. Tubulin polymerization-IN-92 exerts antiproliferative activity, induces G2/M cell cycle arrest and apoptosis in cancer cells. Tubulin polymerization-IN-92 inhibits tumor growth in mouse xenograft models. Tubulin polymerization-IN-92 can be used for the research of colon cancer, cervical cancer, and Paclitaxel (HY-B0015)-resistant ovarian cancer[1].

体外研究
(In Vitro)

Tubulin polymerization-IN-92 (compound 8h) 可强效抑制 HCT116、HeLa、A2780S、A2780T、HT29 和 HUVEC 细胞的增殖，其 IC50 值分别为 3.5、2.4、15.7、22.1 和 7.3 nM，且对 Paclitaxel 耐药的 A2780T 细胞具有活性[1]。
Tubulin polymerization-IN-92 (5 μM; 5 min) 可在体外抑制微管蛋白聚合[1]。
Tubulin polymerization-IN-92 (10-30 nM; 24 h) 可破坏 HT29、A2780S 和 A2780T 细胞中的微管网络[1]。
Tubulin polymerization-IN-92 (10-100 nM; 48 h) 可在 HT29 细胞中以浓度依赖的方式诱导 G2/M 期阻滞[1]。
Tubulin polymerization-IN-92 (30-100 nM; 48 h) 可诱导 HeLa 细胞发生晚期凋亡[1]。
Tubulin polymerization-IN-92 (10-100 nM; 14 days) 可抑制 A2780S、A2780T 和 HT29 细胞的集落形成[1]。

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

Tubulin polymerization-IN-92 相关抗体:

Immunofluorescence[1]

Cell Line: HT29, A2780S, A2780T
Concentration: 10; 30 nM
Incubation Time: 24 h
Result: Induced microtubule depolymerization in HT29, A2780S, and A2780T cells.
Showed intact, organized microtubule networks in untreated cells.

Cell Cycle Analysis[1]

Cell Line: HT29
Concentration: 10, 30, 100 nM
Incubation Time: 48 h
Result: Induced G2/M phase arrest in a concentration-dependent manner.
Increased the proportion of cells in G2/M phase from 8.14% (control) to 60.58% at 100 nM.

Apoptosis Analysis[1]

Cell Line: HeLa
Concentration: 10, 30, 100 nM
Incubation Time: 48 h
Result: Induced late-stage apoptosis in HeLa cells.
Exhibited 8.43% of late apoptotic cells at 30 nM.
Increased late apoptotic cells from 0.47% (control) to 25.12% at 100 nM.

Cell Proliferation Assay[1]

Cell Line: HT29, A2780S, A2780T
Concentration: 40, 100 nM
Incubation Time: 14 days
Result: Significantly decreased the colony number and area of A2780S cells at 40 nM.
Completely inhibited colony formation in A2780T and HT29 cells at 100 nM.
Inhibited colony formation in A2780S
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 CL AUC0-t Cmax Tmax Vss F
Mice[1] 5 mg/kg i.v. 7.02 h 0.28 L/h/kg 16670.37 μg/L·h 1983.65 μg/L 0.39 h 2.63 L/kg 41.56 %
Mice[1] 10 mg/kg p.o. 6.00 h 0.76 L/h/kg 13856.37 μg/L·h 2139.89 μg/L 0.33 h 6.82 L/kg /
体内研究
(In Vivo)

Tubulin polymerization-IN-92 (compound 8h) (5、10 mg/kg；口服；每日 1 次；连续 10 天) 在小鼠 HT29 异种移植模型中表现出抗肿瘤活性[1]。

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

Animal Model: Female Balb/c mice (5-6 weeks) injected with HT-29 cells[1]
Dosage: 5; 10 mg/kg
Administration: p.o.; once daily; 10 days
Result: Exerted favorable in vivo antitumor activity with tumor growth inhibition (TGI) rates of 58.6% and 70.1% at 5 and
10 mg/kg, respectively.
Showed no significant body weight changes at 5 mg/kg dose.
Exhibited severe toxic side
effect at 10 mg/kg.
分子量

533.61

Formula

C31H33F2N3O3
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

Tubulin polymerization-IN-92 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:

Tubulin polymerization-IN-92Microtubule/TubulinApoptosisHCT116A2780THeLapaclitaxel-resistant ovarian cancercolon cancercolchicine siteα-tubulinβ-tubulinA2780Scervical cancerInhibitorinhibitorinhibit

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：
Tubulin polymerization-IN-92
目录号：
HY-183329
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