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

Antitumor agent-77 

Cat. No.: HY-151429
Handling Instructions

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.

For research use only. We do not sell to patients.

Antitumor agent-77 Chemical Structure

Antitumor agent-77 Chemical Structure

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Description

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

 

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.

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.
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.
Molecular Weight

455.25

Formula

C7H11F3N2O5Pt

SMILES

[NH3][Pt]1(OC(C2(C(O1)=O)CC(C(F)(F)F)(C2)O)=O)[NH3]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Product Name:
Antitumor agent-77
Cat. No.:
HY-151429
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