Antitumor agent-83

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Antitumor agent-83 is an activator of pro-apoptotic protein BAX and has significant anti-proliferation effect on tumor cells. Antiumor agent-83 mediates cell Apoptosis by inducing the conformational activation of BAX and has inhibitory effect on A549 cell cycle. Antiumor agent-83 has good metabolic stability and CYPs spectrum in vitro.

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Antitumor agent-83 Chemical Structure

CAS No. : 3038789-74-8

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Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	2.15 μM Compound: 6d	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 36680883]
HCT-116	GI₅₀	3.31 μM Compound: 6d	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 36680883]
K562	GI₅₀	1.41 μM Compound: 6d	Antiproliferative activity against human K562 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by trypan blue cell counting analysis Antiproliferative activity against human K562 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by trypan blue cell counting analysis	[PMID: 36680883]
MDA-MB-231	GI₅₀	3.98 μM Compound: 6d	Antiproliferative activity against human MDA-MB-231 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 36680883]
MV4-11	GI₅₀	2.84 μM Compound: 6d	Antiproliferative activity against human MV4-11 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by trypan blue cell counting analysis Antiproliferative activity against human MV4-11 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by trypan blue cell counting analysis	[PMID: 36680883]
NCI-H1581	GI₅₀	2.15 μM Compound: 6d	Antiproliferative activity against human NCI-H1581 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1581 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 36680883]
PC-3	GI₅₀	2.5 μM Compound: 6d	Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 36680883]
THP-1	GI₅₀	2.18 μM Compound: 6d	Antiproliferative activity against human THP-1 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by trypan blue cell counting analysis Antiproliferative activity against human THP-1 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by trypan blue cell counting analysis	[PMID: 36680883]

In Vitro

Antitumor agent-83 (compound 6d) (5-40 µM; 24 h) activates BAX and mediates cell apoptosis, promotes the release cytochrome c in a dose-dependent manner^[1].
Antitumor agent-83 has significant anti-proliferation effect on A549, HCT-116, PC-3, H1581, MDA-MB-231, K562, MV4-11 and THP-1 tumor cells with GI₅₀ values of 2.15 µM, 3.31 µM, 2.50 µM, 2.15 µM, 3.98 µM, 1.41 µM, 2.84 µM, 2.18 µM, respectively^[1].
Antitumor agent-83 (1-5 µM; 24, 48 and 72h) significantly reduces the viability of A549 cells in a dose-and time-dependent manner^[1].
Antitumor agent-83 (5 µM and 10 µM; 48 h) promotes A549 cells apoptosis in a dose-dependent manner^[1].
Antitumor agent-83 (2.5 µM and 5 µM; 48 h) induces cell cycle arrest in G0/G1 phase with dose-dependent manner^[1].

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

Western Blot Analysis^[1]

Cell Line:	A549 cells.
Concentration:	5, 10, 20 and 40 µM.
Incubation Time:	24 h.
Result:	Significantly up-regulated the expression level of BAX, activated the conformation of BAX and caused the release of cytochrome c.

Cell Viability Assay^[1]

Cell Line:	A549 cells.
Concentration:	1, 2, 3, 4 and 5 µM.
Incubation Time:	24, 48 and 72h.
Result:	Showed inhibitory effect on the growth of A549 cells and exhibited greatest impact on the viability of A549 cells (5 µM; 72 h).

Apoptosis Analysis^[1]

Cell Line:	A549 cells.
Concentration:	5 and 10 µM.
Incubation Time:	48 h.
Result:	Showed active effect on the apoptosis of A549 cells with cell apoptosis were 15.43 % and 73.40 % at the concentration of 5 µM and 10 µM, respectively.

Cell Cycle Analysis^[1]

Cell Line:	A549 cells.
Concentration:	2.5 and 5 µM.
Incubation Time:	48 h.
Result:	Exhibited inhibitory effect on A549 cell cycle.

Molecular Weight

494.59

Formula

C₂₉H₃₀N₆O₂

CAS No.

3038789-74-8

SMILES

CN(C1CCN(CC1)C(C2=CC=C(C=C2)N3N=C(/C(C3=O)=N/NC4=CC=CC=C4)C5=CC=CC=C5)=O)C

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]. Zhang Z, et al. Optimization of BAX trigger site activator BTSA1 with improved antitumor potency and in vitro ADMET properties. Eur J Med Chem. 2023 Feb 15;248:115076. [Content Brief]