Antitumor agent-53

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Antitumor agent-53 is a potent antitumor agent. Antitumor agent-53 induces cell cycle arrest at the G2/M phase. Antitumor agent-53 inhibits the PI3K/AKT pathway to induce the apoptosis of HGC-27 cells. Antitumor agent-53 has the potential for the research of gastrointestinal tumors.

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

Antitumor agent-53 Chemical Structure

CAS No. : 2757145-67-6

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Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	7.87 μM Compound: 6f	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 34990980]
GES1	IC₅₀	12.74 μM Compound: 6c	Antiproliferative activity against human GES1 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human GES1 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 34774339]
GES1	IC₅₀	3.1 μM Compound: 6f	Antiproliferative activity against human GES1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human GES1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 34990980]
HepG2	IC₅₀	> 18 μM Compound: 6f	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 34990980]
HGC-27	IC₅₀	0.37 μM Compound: 6f	Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 34990980]
HGC-27	IC₅₀	2.5 μM Compound: 6c	Antiproliferative activity against human HGC-27 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human HGC-27 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 34774339]
HT-29	IC₅₀	4.01 μM Compound: 6f	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 34990980]
MCF7	IC₅₀	9.11 μM Compound: 6f	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 34990980]
MGC-803	IC₅₀	0.27 μM Compound: 6c	Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 34774339]
SGC-7901	IC₅₀	1.67 μM Compound: 6c	Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 34774339]

In Vitro

Antitumor agent-53 (compound 6f) (0, 0.22, 0.67, 2, 6, 18 µM; 72 h) shows anti-proliferation activity with IC₅₀s of 3.10, 0.37, 4.01, >18, 7.87, 9.11 µM for HGC-27, HT-29, HepG-2, A549, MCF7, GES-1 cells^[1].
Antitumor agent-53 (0.15, 0.3, 0.6 µM) shows anti-proliferative activity in HGC-27 and HT-29 cells with a dose-dependent manner^[1].
Antitumor agent-53 (100, 200 µM) shows a certain inhibitory activity against Topo I at 200 μM^[1].
Antitumor agent-53 (0.1, 0.3, 0.9 μM; 24 h) induces cell cycle arrest at the G2/M phase in HGC-27, HT-29 cells^[1].
Antitumor agent-53 (0.1, 0.3, 0.9, 2.7 μM; 24 h) induces the apoptosis of HGC-27 and HT-29 cells in a concentration-dependent manner^[1].
Antitumor agent-53 (0.15, 0.3, 0.6 μM; 24 h) inhibits the migration and invasion of HGC-27 cells in a concentration-dependent manner^[1].
Antitumor agent-53 (0.1, 0.3, 0.9 μM; 24 h) suppresses the PI3K/AKT pathway to induce the apoptosis of HGC-27 cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	HGC-27, HT-29, HepG-2, A549, MCF7, GES-1 cells
Concentration:	0, 0.22, 0.67, 2, 6, 18 µM
Incubation Time:	72 h
Result:	Showed anti-proliferation activity with IC₅₀s of 3.10, 0.37, 4.01, >18, 7.87, 9.11 µM for HGC-27, HT-29, HepG-2, A549, MCF7, GES-1 cells.

Cell Cycle Analysis^[1]

Cell Line:	HGC-27, HT-29 cells
Concentration:	0.1, 0.3, 0.9 μM
Incubation Time:	24 h
Result:	Cells were arrest at the G2/M phase.

Apoptosis Analysis^[1]

Cell Line:	HGC-27, HT-29 cells
Concentration:	0.1, 0.3, 0.9, 2.7 μM
Incubation Time:	24 h
Result:	Induced the apoptosis of HGC-27 and HT-29 cells in a concentration-dependent manner.

Western Blot Analysis^[1]

Cell Line:	HGC-27 cells
Concentration:	0.1, 0.3, 0.9 μM
Incubation Time:	24 h
Result:	Suppressed the PI3K/AKT pathway to induce the apoptosis of HGC-27 cells.

Molecular Weight

383.42

Formula

C₂₄H₁₈FN₃O

CAS No.

2757145-67-6

SMILES

O=C1C2=C(N(C3C4=C(C5=CC=CC=C5N4)CCN13)C6=CC=CC(F)=C6)C=CC=C2

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

Handling Instructions (2659 KB)

References

[1]. Hao X, et al. Design, synthesis and bioactivity evaluation of novel N-phenyl-substituted evodiamine derivatives as potent anti-tumor agents. Bioorg Med Chem. 2021; 55:116595. [Content Brief]