1. Apoptosis Protein Tyrosine Kinase/RTK
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  3. Antitumor agent-55

Antitumor agent-55 (compound 5q) is a potent antitumor agent. Antitumor agent-55 effectively inhibits PC3, with an IC50 of 0.91 μM. Antitumor agent-55 effectively inhibits the colony formation, suppresses the cell migration in PC3. Antitumor agent-55 induces G1/S phase arrest and apoptosis in PC3.

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Antitumor agent-55 Chemical Structure

Antitumor agent-55 Chemical Structure

CAS No. : 2522594-49-4

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Description

Antitumor agent-55 (compound 5q) is a potent antitumor agent. Antitumor agent-55 effectively inhibits PC3, with an IC50 of 0.91 μM. Antitumor agent-55 effectively inhibits the colony formation, suppresses the cell migration in PC3. Antitumor agent-55 induces G1/S phase arrest and apoptosis in PC3[1].

Cellular Effect
Cell Line Type Value Description References
MCF7 IC50
11.54 μM
Compound: 5q
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 24 to 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 24 to 72 hrs by MTT assay
[PMID: 32619887]
MGC-803 IC50
8.21 μM
Compound: 5q
Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability after 24 to 72 hrs by MTT assay
Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability after 24 to 72 hrs by MTT assay
[PMID: 32619887]
PC-3 IC50
0.91 μM
Compound: 5q
Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 24 to 72 hrs by MTT assay
Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 24 to 72 hrs by MTT assay
[PMID: 32619887]
PC-9 IC50
34.68 μM
Compound: 5q
Antiproliferative activity against human PC9 cells assessed as reduction in cell viability after 24 to 72 hrs by MTT assay
Antiproliferative activity against human PC9 cells assessed as reduction in cell viability after 24 to 72 hrs by MTT assay
[PMID: 32619887]
In Vitro

Antitumor agent-55 (compound 5q) shows inhibitory activity against MCF-7, PC3, MGC-803, PC9, and WPMY-1 (normal human prostatic stromal myofibroblast cell line), with IC50 values of 11.54 ± 0.18, 0.91 ± 0.31, 8.21 ± 0.50, 34.68 ± 0.67, and 48.15 ± 0.33, respectively[1].
Antitumor agent-55 (0-10 μM, 24-72 h) significantly inhibits the proliferation of PC3 cells dose- and time-dependently[1].
Antitumor agent-55 (0-4 μM, 24 h) increases the G1/S phase population, and dose-dependently elevates the expression of p27 protein[1].
Antitumor agent-55 (0-4 μM, 24-48 h) dose-dependently induces the accumulation of ROS, and induces apoptosis of PC3 cells through activating the two apoptotic signaling pathways simultaneously[1].
Antitumor agent-55 (0-1 μM, 48 h) effectively inhibits the wound healing and the migration of PC3 cells in a dose-dependent manner[1].

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

Cell Viability Assay

Cell Line: PC3 cells[1]
Concentration: 0, 0.156, 0.313, 0.625, 1.25, 2.5, 5, 10 μM
Incubation Time: 24, 48, 72 h
Result: Significantly inhibited the proliferation of PC3 cells dose- and time-dependently, formed fewer and smaller colonies.

Cell Cycle Analysis

Cell Line: PC3 cells[1]
Concentration: 0, 1, 2, 4 μM
Incubation Time: 24 h
Result: Significantly increased the G1/S phase population while decreased G2/M content at high concentration in PC3 cells.

Western Blot Analysis

Cell Line: PC3 cells[1]
Concentration: 0, 1, 2, 4 μM
Incubation Time: 24 h, 48 h
Result: Dose-dependently elevated the expression of p27 protein, markedly elevated the expression of pro-apoptotic Bax and P53 while anti-apoptotic Bcl-2 expression was down-regulated, and significantly increased the expression of cleaved caspase 3/9 and cleaved PARP in a dose-dependent manner.

Apoptosis Analysis

Cell Line: PC3 cells[1]
Concentration: 0, 1, 2, 4 μM
Incubation Time: 48 h
Result: Dose-dependently led to significant increase of apoptotic population, and the apoptotic percentage was up to 70.7% at 4 μM, which was far higher than the control group (3.5%).
Molecular Weight

598.72

Formula

C32H34N6O4S

CAS No.
SMILES

O=C(NC1CN(C2=CC(C)=NC3=NC(SCC4=C5C=CC=CC5=CC=C4)=NN23)CCC1)C6=CC(OC)=C(OC)C(OC)=C6

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

Purity & Documentation
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Antitumor agent-55
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HY-146038
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