1. Apoptosis
  2. Apoptosis
  3. Tetrazanbigen

Tetrazanbigen is a potent and selective antitumor agent. Tetrazanbigen exhibits strong antitumor efficacy against six human cancer cell lines with an IC50 range of 2.13-8.01 μg/mL and an IC50 of 11.25 μg/mL against normal hepatocytes. Tetrazanbigen induces S phase arrest and apoptosis in QGY-7701 cells. Tetrazanbigen exerts its antitumor activity by inducing lipid accumulation accumulation in cancer cells.

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Tetrazanbigen Chemical Structure

Tetrazanbigen Chemical Structure

CAS No. : 2121990-04-1

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Description

Tetrazanbigen is a potent and selective antitumor agent. Tetrazanbigen exhibits strong antitumor efficacy against six human cancer cell lines with an IC50 range of 2.13-8.01 μg/mL and an IC50 of 11.25 μg/mL against normal hepatocytes. Tetrazanbigen induces S phase arrest and apoptosis in QGY-7701 cells. Tetrazanbigen exerts its antitumor activity by inducing lipid accumulation accumulation in cancer cells[1].

In Vitro

Tetrazanbigen (0-12 μg/mL, 72 h) inhibits the proliferation of QGY-7701 cells, BIU-87 cells, Hep-2 cells, SGC-7901 cells, K562 cells, SW626 cells, and LO2 cells, with IC50 values of 2.13 μg/mL, 3.25 μg/mL, 3.84 μg/mL, 4.41 μg/mL, 7.70 μg/mL, 8.01 μg/mL, and 11.25 μg/mL, respectively[1].

Tetrazanbigen (0-8 μg/mL, 24-72 h) induces lipid accumulation in QGY-7701 cells[1].

Tetrazanbigen (2-4 μg/mL, 72 h) induces QGY-7701 cell cycle arrest at S phase and apoptosis[1].

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

Cell Cycle Analysis[1]

Cell Line: QGY-7701 cells
Concentration: 2 μg/mL, 4 μg/mL
Incubation Time: 72 h
Result: Increased the population of S phase, decreased the populations of G0/G1 phases.

Apoptosis Analysis[1]

Cell Line: QGY-7701 cells
Concentration: 4 μg/mL
Incubation Time: 72 h
Result: Induced apoptosis, and caused condensed nuclei, apoptotic bodies and cellular shrinkage, chromatin margination.
Caused the appearance of a large number of lipid droplets.
In Vivo

Tetrazanbigen (1.5 mg/kg/day, i.p., 5 weeks) inhibits tumor growth in nude mice and has good safety[1].

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

Animal Model: Nude mice (Female athymic of 4 weeks old) bearing xenografts of QGY-7701 cell line (5 × 106, s.c.) [1]
Dosage: 1.5 mg/kg/day
Administration: i.p., 5 weeks
Result: Reduced tumor volume and inhibited tumor weight, the TGI based on tumor weight was 87%.
Molecular Weight

288.35

Formula

C18H16N4

CAS No.
SMILES

C1(N=C2N3CCC4=C(C=CC=C4)C3CN=C2N5)=C5C=CC=C1

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Purity & Documentation
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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.

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Tetrazanbigen
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HY-176249
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