2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. Antitumor agent-138

Antitumor agent-138 (compound 5b) 是一种作用在微管蛋白 (tubulin) colchicine 结合位点的微管蛋白聚合抑制剂，IC50 为 1.87 μM。Antitumor agent-138 在 G2/M 期阻滞细胞周期并且诱导 MCF-7 细胞自噬 (apoptosis)。Antitumor agent-138 抑制细胞迁移和血管形成。

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Antitumor agent-138 Chemical Structure

Antitumor agent-138 Chemical Structure

CAS No. : 2975168-22-8

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Antitumor agent-138 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

Antitumor agent-138 (compound 5b) is an inhibitor against tubulin polymerization at tubulin colchicine-binding sites, with IC50 of 1.87 μM. Antitumor agent-138 arrests the cell cycle at G2/M phase and induces an apoptosis in MCF-7 cells. Antitumor agent-138 inhibits cells migration and angiogenesis[1].

体外研究
(In Vitro)

Antitumor agent-138 在细胞 MCF-7，A549，MDA-MB-231，HT-29，HeLa 和 L02 中表现出抗增殖活性， IC50 值分别是 0.04，0.39，0.04，0.06，0.11 和 2.73 μM[1]。
Antitumor agent-138 (5-20 nM) 抑制人乳腺癌细胞 MCF-7 集落的形成[1]。
Antitumor agent-138 (25-200 nM) 诱导 MCF-7 中微管蛋白崩溃[1]。
Antitumor agent-138 (6.25-50 nM) 剂量依赖地抑制 HUVEC 细胞成管，抑制血管形成[1]。

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

Antitumor agent-138 相关抗体:

Cell Migration Assay [1]

Cell Line: A549
Concentration: 6.25-50 nM
Incubation Time: 24 h
Result: Inhibited the cell migration in a dose-dependent manner.

Cell Proliferation Assay[1]

Cell Line: MCF-7, A549, MDA-MB-231, HT-29, HeLa and L02
Concentration: 0-5 μM
Incubation Time: 48 h
Result: Exhibited anti-proliferative properties in cancer cells MCF-7, A549, MDA-MB-231, HT-29, HeLa with low concentrations in nanomole.

Western Blot Analysis[1]

Cell Line: MCF-7
Concentration: 6.25-25 nM
Incubation Time: 24 h
Result: Increased P21, Cyclin B1, Cdc25c and cdk7 in a dose- and time-dependent manner.
Increased Bax, Cleaved-PARP, Bim and Cleaved Caspase-9, decreasesd Bcl-2 in a dose- and time-dependent manner.

Immunofluorescence[1]

Cell Line: MCF-7
Concentration: 25-200 nM
Incubation Time: 8 h
Result: Disrupted the microtubule network into punctate.
体内研究
(In Vivo)

Antitumor agent-138 (20 mg/kg，腹腔注射，21 天) 在 MCF-7 异种移植 BALB/c 裸鼠体内表现出肿瘤抑制活性，肿瘤生长抑制率为 68.95%[1]。

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

Animal Model: MCF-7 xenograft in BALB/c nude mice[1]
Dosage: 20 mg/kg
Administration: intraperitoneal injection for 21 days
Result: Inhibited the tumor growth with TGI of 68.95%
分子量

367.40

Formula

C20H21N3O4
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

Antitumor agent-138 相关分类

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  • 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:

Antitumor agent-1382975168-22-8Antitumor agent138Antitumor agent 138Microtubule/TubulinApoptosistubulin colchicine-binding sitesMCF-7 xenograftBALB/c nude miceMCF-7A549Inhibitorinhibitorinhibit

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