Antiproliferative agent-5

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Antiproliferative agent-5 (compound 4o) can significantly and irreversibly inhibit proliferation of gastric cancer cells. Antiproliferative agent-5 causes the G2/M phase arrest, and induces ROS accumulation and activation of autophagy. Antiproliferative agent-5 can be used for researching anticancer.

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

Antiproliferative agent-5 Chemical Structure

CAS No. : 2459892-41-0

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

ROS, Autophagy^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	> 10 μM Compound: 4o	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth at measured after 72 hrs by SRB assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth at measured after 72 hrs by SRB assay	[PMID: 32683165]
BGC-823	GI₅₀	0.64 μM Compound: 4o	Antiproliferative activity against human BGC-823 cells assessed as inhibition of cell growth at measured after 72 hrs by SRB assay Antiproliferative activity against human BGC-823 cells assessed as inhibition of cell growth at measured after 72 hrs by SRB assay	[PMID: 32683165]
EJ	GI₅₀	> 10 μM Compound: 4o	Antiproliferative activity against human EJ cells assessed as inhibition of cell growth at measured after 72 hrs by SRB assay Antiproliferative activity against human EJ cells assessed as inhibition of cell growth at measured after 72 hrs by SRB assay	[PMID: 32683165]
HGC-27	GI₅₀	0.64 μM Compound: 4o	Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth at measured after 72 hrs by SRB assay Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth at measured after 72 hrs by SRB assay	[PMID: 32683165]
MGC-803	GI₅₀	0.64 μM Compound: 4o	Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth at measured after 72 hrs by SRB assay Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth at measured after 72 hrs by SRB assay	[PMID: 32683165]
MKN-45	GI₅₀	0.64 μM Compound: 4o	Antiproliferative activity against human MKN-45 cells assessed as inhibition of cell growth at measured after 72 hrs by SRB assay Antiproliferative activity against human MKN-45 cells assessed as inhibition of cell growth at measured after 72 hrs by SRB assay	[PMID: 32683165]
SGC-7901	GI₅₀	0.64 μM Compound: 4o	Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell growth at measured after 72 hrs by SRB assay Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell growth at measured after 72 hrs by SRB assay	[PMID: 32683165]
SW-620	IC₅₀	0.058 μM Compound: 24	Reversal of resistance to paclitaxel-induced cytotoxicity in human SW-620/AD300 cells assessed as reduction in paclitaxel IC50 at 1 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 4.23 +/- 0.50 uM) Reversal of resistance to paclitaxel-induced cytotoxicity in human SW-620/AD300 cells assessed as reduction in paclitaxel IC50 at 1 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 4.23 +/- 0.50 uM)	[PMID: 34723530]

Molecular Weight

597.49

Formula

C₂₈H₂₁BrN₈OS

CAS No.

2459892-41-0

SMILES

O=C(C1=CC=C(NC2=CC(C)=NC3=NC(SCC4=NC5=CC=CC=C5N4)=NN23)C=C1)/C=C/C6=NC(Br)=CC=C6

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]. Wang S, et al. Discovery of new [1,2,4] Triazolo[1,5-a]Pyrimidine derivatives that Kill gastric cancer cells via the mitochondria pathway. Eur J Med Chem. 2020;203:112630. [Content Brief]