2. Apoptosis Immunology/Inflammation
  3. Apoptosis Ferroptosis Bcl-2 Family COX
  4. Antitumor agent-77

Antitumor agent-77 具有抗肿瘤活性，能抑制癌细胞的生长和迁移。Antitumor agent-77 通过抑制 GPx-4 和升高 COX2 引发铁死亡 (ferroptosis)。Antitumor agent-77 还能激活肿瘤细胞固有凋亡通路 (Bax-Bcl-2-caspase-3)，阻碍肿瘤细胞上皮间质转化 (EMT) 过程。

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Antitumor agent-77 Chemical Structure

Antitumor agent-77 Chemical Structure

CAS No. : 2870703-21-0

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Antitumor agent-77 相关抗体

Top Publications Citing Use of Products

查看 Bcl-2 Family 亚型特异性产品:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

查看 COX 亚型特异性产品:

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COX COX-1 COX-2 COX-3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Antitumor agent-77 is an antitumor agent, inhibits cancer cells growth and migration. Antitumor agent-77 triggers ferroptosis by inhibiting GPx-4 and elevating COX2. Antitumor agent-77 also activates intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and hinders Epithelial-mesenchymal transition (EMT) process of cancer cells[1].

IC50 & Target

COX-2

 

Bax

 

Bcl-2

 

体外研究
(In Vitro)

Antitumor agent-77 (compound 2a) (30 μM; 4 h) exhibits better solubility and improved cellular uptake than Carboplatin (HY-17393) in A549 cells[1].
Antitumor agent-77 (20 μM; 36 h) produces cytotoxicity by inducing apoptosis of A549 cancer cells[1].
Antitumor agent-77 (20 μM; 24 h) results in significant down-regulation of Bcl-2 and upregulation of Bax, also leads to E-cadherin increase, Vimentin decrease[1].
Antitumor agent-77 (20 μM; 24 h) arrests cell cycle at S phase and G2/M phase[1].
Antitumor agent-77 (10 μM; 12 h) inhibits cells migration with inhibition rate of 52%[1].

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

Antitumor agent-77 相关抗体:

Apoptosis Analysis[1]

Cell Line: A549 cells
Concentration: 20 μM
Incubation Time: 36 hours
Result: Resulte cell apopsotsis with average apoptotic values (including both early and late apoptotic states which were displayed in Q1-LR and Q1-UR, respectively) of 25.34%.

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 20 μM
Incubation Time: 24 hours
Result: Elevated the level of cleaved caspase-3 and reduced the level of caspase-3 in A549 cells.
Decreased anti-apoptotic protein Bcl-2 and increased pro-apoptotic protein Bax.
Elevated the expression of E-cadherin and on the other hand, lowered the protein level of Vimentin.

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 20 μM
Incubation Time: 24 hours
Result: Blocked cell cycle progression in S and G2/M phase with the values of 41.11% and 26.03%, respectively.
体内研究
(In Vivo)

Antitumor agent-77 (compound 2a) (6 μg/kg; i.v.; injected on day 8, 10, 12) exhibits similar potency compared with Oxaliplatin (HY-17371), without significant damage to kidney and liver as well as weight loss[1].

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

Animal Model: A549 xenograft models in mouse[1]
Dosage: 6 μg/kg
Administration: Intravenous injection; administration on day 8, 10, 12 after establishing xenograft models (A549 cells; s.c.)
Result: Significantly repressed tumor growth, and maintained normal kidney and liver architecture in mice.
分子量

455.25

Formula

C7H11F3N2O5Pt
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-77 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-772870703-21-0Antitumor agent77Antitumor agent 77ApoptosisFerroptosisBcl-2 FamilyCOXCyclooxygenaseantitumormigrationGPx-4COX2apoptotic pathwayBax-Bcl-2-caspase-3Epithelial-mesenchymal transitionEMTliposolubleA549Inhibitorinhibitorinhibit

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