2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. Microtubule/Tubulin Apoptosis Reactive Oxygen Species
  4. Tubulin polymerization-IN-6

Tubulin polymerization-IN-6 (化合物 5f) 是一种有效的微管蛋白聚合抑制剂，其IC50 为 1.09 μM。Tubulin polymerization-IN-6 抑制细胞迁移和管的形成，并有助于抗血管生成。Tubulin polymerization-IN-6 可显著抑制 HT29 移植 Balb/c 裸鼠肿瘤生长。

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Tubulin polymerization-IN-6 Chemical Structure

Tubulin polymerization-IN-6 Chemical Structure

CAS No. : 2768613-52-9

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Tubulin polymerization-IN-6 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-6 (compound 5f) is a potent tubulin polymerization inhibitor, with an IC50 of 1.09 μM. Tubulin polymerization-IN-6 inhibits cell migration and tube formation and contributes to the anti-angiogenesis. Tubulin polymerization-IN-6 can greatly inhibit tumor growth on HT29 xenograft Balb/c nude mice[1].

IC50 & Target

IC50: 1.09 μM (Tubulin polymerization)[1]
体外研究
(In Vitro)

Tubulin polymerization-IN-6 (compound 5f) (0-20 μM, 24 h) shows a broad spectrum of anti-proliferation activity against cancer cell lines[1].
Tubulin polymerization-IN-6 (0-100 nM, 24 h) inhibits tumor cells colony formation, up-regulates the expression of Ac-α-tubulin and DeY-α-tubulin [1].
Tubulin polymerization-IN-6 (0-5 μM, 1 h) competes with colchicine and directly binds to the colchicine binding site, thus inhibit tubulin polymerization[1].
Tubulin polymerization-IN-6 (0-250 nM, 24 h) possesses a favorable anti-migration activity against cancer cells[1].
Tubulin polymerization-IN-6 (0-50 nM, 24 h) has the ability to inhibit the angiogenesis of HUVEC cells[1].
Tubulin polymerization-IN-6 (0-100 nM, 24 h) induces cell cycle arrest by regulating associated proteins, induces apoptosis by regulating associated proteins and down-regulating mitochondrial membrane potential, and dose-dependently promotes the production of ROS in HT29 cells[1].

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

Tubulin polymerization-IN-6 相关抗体:

Cell Proliferation Assay

Cell Line: HT29, MCF-7, HeLa, MDA-MB-231, A549[1]
Concentration: 0-20 μM
Incubation Time: 24 h
Result: Had a broad spectrum of anti-proliferation activity against cancer cell lines (MCF-7, MDA-MB-231, A549, Hela, and HT29), with IC50 values of 0.14 ± 0.03, 0.10 ± 0.00, 0.24 ± 0.03, 0.035 ± 0.002, and 0.023 ± 0.001 μM, respectively; and showed moderate anti-proliferative activity against drug resistant cancer cells (MCF-7/TxR and A549/TxR), with IC50 values of 0.18 ± 0.02 and 0.31 ± 0.08 μM, and DRI (drug-resistant index) of 1.3 and 1.2, respectively.

Western Blot Analysis

Cell Line: HT29 cells[1]
Concentration: 0, 25, 50, and 100 nM
Incubation Time: 24 h
Result: Up-regulated the expression of Ac-α-tubulin (acetyl-α-tubulin) and DeY-α-tubulin (detyrosinated-α-tubulin); regulated the expressions of the proteins involved in cell cycle such as cdc25c, cdk7, cyclin B1, and cdc2; down-regulated the level of Bim and up-regulated the levels of Bcl-2, p-Bcl-2, and Bax, decreased the expression of p-Histone H3(Ser10) and increased the expression of cleaved-Caspase-9, cleaved-Caspase-3, PARP, and cleaved-PARP.

Immunofluorescence

Cell Line: HT29 cells[1]
Concentration: 0, 25, 50, and 100 nM
Incubation Time: 6 h
Result: Dose-dependently depolymerized the tubulin polymers into oligomers, and caused the microtubule network to collapse in HT29 cells.

Cell Cycle Analysis

Cell Line: HT29 cells[1]
Concentration: 0, 12.5, 25, 50, and 100 nM
Incubation Time: 24 h
Result: Induced a dose dependent G2/M phase arrest, increased the proportion of G2/M phase cells from 20.9% to 87.5% at 100 nM.

Apoptosis Analysis

Cell Line: HT29 cells[1]
Concentration: 0, 25, 50, and 100 nM
Incubation Time: 24 h
Result: Induced apoptosis, increased the percentages of total apoptosis cells, down-regulated mitochondrial membrane potential.
体内研究
(In Vivo)

Tubulin polymerization-IN-6 (compound 5f) (HT29 xenograft Balb/c nude mice, 0-10 mg/kg, IP, once every two days, for three weeks) dose-dependently inhibits the tumor growth[1].
Tubulin polymerization-IN-6 (SD rats, 10 mg/kg, IV, once) shows the better pharmacokinetic properties[1]. Pharmacokinetic Parameters of Tubulin polymerization-IN-6 in SD rats[1].

Parameters 5f
t1/2 (h) 1.73
AUC (μg/L·h) 5.67
MRT (h) 1.92
CL (L/h/kg) 1.76
Tmax (h) 0.14
Cmax (ng/mL) 6.88

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

Animal Model: Immunodeficient Balb/c nude mice (HT29 xenograft, 5-week-old, 36 mice, six groups)[1]
Dosage: 0, 5, 7.5, 10 mg/kg
Administration: IP, once every two days, for three weeks
Result: Dose-dependently inhibited the tumor growth, inhibits the tumor weight growth by 75.5% at 10 mg/kg.
Animal Model: SD rats (5-week-old)[1]
Dosage: 10 mg/kg
Administration: IV, once (Pharmacokinetic Analysis)
Result: Showed the better pharmacokinetic properties, exhibited an eight-fold half-life and a two-fold AUC improvement.
分子量

375.37

Formula

C19H21NO7
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

Tubulin polymerization-IN-6 相关分类

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Keywords:

Tubulin polymerization-IN-62768613-52-9Microtubule/TubulinApoptosisReactive Oxygen SpeciesHT29 cellsLow toxicityAntitumor activityInhibitorinhibitorinhibit

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