2. Apoptosis Cytoskeleton Cell Cycle/DNA Damage
  3. Apoptosis Microtubule/Tubulin
  4. αβ-Tubulin-IN-1

αβ-Tubulin-IN-1 是一种有效且具有口服活性的 αβ-Tubulin 抑制剂。αβ-Tubulin-IN-1 诱导细胞周期停滞在 G2/M 期和诱导细胞凋亡 (apoptosis)。αβ-Tubulin-IN-1 抑制肿瘤细胞迁移和转移。αβ-Tubulin-IN-1 以剂量依赖性方式显示出显着的抗肿瘤功效。

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

αβ-Tubulin-IN-1 Chemical Structure

αβ-Tubulin-IN-1 Chemical Structure

CAS No. : 2478584-74-4

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

αβ-Tubulin-IN-1 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

αβ-Tubulin-IN-1 is a potent and orally active αβ-Tubulin inhibitor. αβ-Tubulin-IN-1 induces cell cycle arrest at G2/M and efficient apoptosis. αβ-Tubulin-IN-1 inhibits tumor cell migration and Metastasis. αβ-Tubulin-IN-1 shows significant antitumor efficacy in a dose dependent manner[1].

IC50 & Target

αβ-Tubulin[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A2780/Taxol IC50
13.1 nM
Compound: 12b
Cytotoxicity in human A2780T assessed as inhibition in cell growth measured after 24 hrs by MTT assay
Cytotoxicity in human A2780T assessed as inhibition in cell growth measured after 24 hrs by MTT assay
[PMID: 35084853]
A2780S IC50
16.4 nM
Compound: 12b
Cytotoxicity in human A2780S assessed as inhibition in cell growth measured after 24 hrs by MTT assay
Cytotoxicity in human A2780S assessed as inhibition in cell growth measured after 24 hrs by MTT assay
[PMID: 35084853]
A2780S IC50
8 nM
Compound: 12b
Antiproliferative activity against human A2780S cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Antiproliferative activity against human A2780S cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 35084853]
A549 IC50
60.1 nM
Compound: 12b
Cytotoxicity in human A549 assessed as inhibition in cell growth measured after 24 hrs by MTT assay
Cytotoxicity in human A549 assessed as inhibition in cell growth measured after 24 hrs by MTT assay
[PMID: 35084853]
A549/TR IC50
63.8 nM
Compound: 12b
Cytotoxicity in human A549T assessed as inhibition in cell growth measured after 24 hrs by MTT assay
Cytotoxicity in human A549T assessed as inhibition in cell growth measured after 24 hrs by MTT assay
[PMID: 35084853]
HeLa IC50
5 nM
Compound: 12b
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 35084853]
MCF7 IC50
11.3 nM
Compound: 12b
Cytotoxicity in human MCF7 assessed as inhibition in cell growth measured after 24 hrs by MTT assay
Cytotoxicity in human MCF7 assessed as inhibition in cell growth measured after 24 hrs by MTT assay
[PMID: 35084853]
MCF7 IC50
9 nM
Compound: 12b
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 35084853]
NCI/ADR-RES IC50
13.5 nM
Compound: 12b
Cytotoxicity in human NCI-ADR-RES assessed as inhibition in cell growth measured after 24 hrs by MTT assay
Cytotoxicity in human NCI-ADR-RES assessed as inhibition in cell growth measured after 24 hrs by MTT assay
[PMID: 35084853]
NCI-H460 IC50
14 nM
Compound: 12b
Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 35084853]
Raji IC50
13 nM
Compound: 12b
Antiproliferative activity against human Raji cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Antiproliferative activity against human Raji cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 35084853]
体外研究
(In Vitro)

αβ-Tubulin-IN-1 (compound 12 b) (0, 0.5, 1, 5, 10, 50 µM; 16 h) promotes αβ-tubulin degradation in a concentration-dependent manner in Hela and K562 (0-10 µM) cells[1].
αβ-Tubulin-IN-1 exhibits potent cytotoxic activity toward sensitive cells and resistant cells[1].
αβ-Tubulin-IN-1 (0-300 nM; 48 h) induces cell cycle arrest at G2/M and efficient apoptosis in A2780S and A2780T cells[1].
αβ-Tubulin-IN-1 (0, 1.25, 2.5, 5, 10 nM; 24, 48 h) inhibits tumor cell migration and Metastasis with the inhibition rate of 76.21% and 85.07% for 24 , 48 h in human umbilical vein endothelial cells (HUVEC)[1].

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

αβ-Tubulin-IN-1 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Hela, A2780S, MCF-7, Raji, H460 cells
Concentration: 0-500 nM
Incubation Time: 24 h
Result: Showed anti-proliferative activity with IC50s of 5, 8, 9,13, 14 nM for Hela, A2780S, MCF-7, Raji, H460 cells, respectively.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 10 µM
Incubation Time: 16 h
Result: Remarkably promoted tubulin degradation by binding to the colchicine site, and the degradation process relied on the ubiquitin−proteasome pathway.

Cell Viability Assay[1]

Cell Line: A2780S, A2780T, A549, A549T, MCF7, MCF7/ADR cells
Concentration:
Incubation Time: 24 h
Result: Exhibited potent cytotoxic activity with IC50s of 16.4, 13.1, 60.1, 63.8, 11.3, 13.5 nM for A2780S, A2780T, A549, A549T, MCF7, MCF7/ADR cells, respectively.

Cell Cycle Analysis[1]

Cell Line: A2780S (PTX-sensitive), A2780T ( PTX-resistant) cells
Concentration: 0, 3, 10, 30, 100, 300 nM
Incubation Time: 48 h
Result: Induced cell cycle arrest at G2/M phase with the the percentages of A2780S and A2780T cells were 55.10%, 72.18% at 100 nM, and 79.54%, 72.89% at 300 nM.

Apoptosis Analysis[1]

Cell Line: A2780S, A2780T cells
Concentration: 0, 3, 10, 30, 100, 300 nM
Incubation Time: 48 h
Result: Induced cell apoptosis with the total numbers of late apoptotic cells were 3.7%, 25.2%, 30.6% at 30,100, and 300 nM, and 5.2% % late apoptotic cells in control.
体内研究
(In Vivo)

αβ-Tubulin-IN-1 (5 mg/kg; i.v., p.o.) shows intravenous and oral administration approaches are available in vivo[1].
αβ-Tubulin-IN-1 (10, 20, 40 mg/kg; i.v.; 3 times a week for 2-4 weeks) shows significant antitumor efficacy in a dose dependent manner[1].
Pharmacokinetic Parameters of αβ-Tubulin-IN-1 in rats[1].

route i.v. p.o.
dose (mg/kg) 5 5
T1/2 (h) 3.57±1.10 4.42±1.90
CL (L/h/kg) 1.52±0.39 5.06±1.70
Vss (L/kg) 8.08±4.19 35.26±25.76
AUC0-∞ (µg/mL·h) 3448.81±782.66 1058.74±285.62
Cmax (µg/L) 2601.47±444.20 189.29±119.02
F (%) 30.70
Rats, 5 mg/kg for i.v., 5 mg/kg for p.o.[1].

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

Animal Model: Rats[1]
Dosage: 5 mg/kg
Administration: I.v. or p.o.
Result: Showed oral bioavailability (F=30.70%) with the T1/2 values for intravenous and oral administration approaches are 3.57 h and 4.42 h, respectively.
Animal Model: 5-6weeks female Balb/C and athymic nude mice (A2780S and A2780T Xenograft) Models[1]
Dosage: 10, 20, 40 mg/kg for i.v., 40 mg/kg for p.o.
Administration: I.v.; 3 times a week for 2-4 weeks
Result: Showed significant antitumor efficacy with tumor growth inhibition (TGI) of 66.06%, 71.47% and 92.41% at 10, 20 and 40 mg/kg in A2780S xenograft nude mice model, and 26.94%, 37.2%, 75.73% at 10, 20 and 40 mg/kg in PTX-resistant A2780T xenograft model for i.v. injection, did not show an acceptable antitumor efficacy with 34.93% of TGI at the 40 mg/kg for p.o..
分子量

409.44

Formula

C25H19N3O3
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

αβ-Tubulin-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:

αβ-Tubulin-IN-12478584-74-4ApoptosisMicrotubule/Tubulinorally activeantitumorapoptosisubiquitin?proteasomeG2/MHeLa cellsXenograft modelmigrationInhibitorinhibitorinhibit

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：
αβ-Tubulin-IN-1
目录号：
HY-144132
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