Anticancer agent 84

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Anticancer agent 84 is an anticancer agent. Anticancer agent 84 represses the transcription of c-MYC by stabilizing the G-quadruplex (G4) structure. Anticancer agent 84 can be used for the research of cancer.

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

Anticancer agent 84 Chemical Structure

CAS No. : 2714510-72-0

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Description

IC₅₀ & Target

IC50: 5.0 μM (HepG2); 3.9 μM (MDA-MB-231); ＞100 μM (HBL-100)^[1]

In Vitro

Anticancer agent 84 has cytotoxicity in cancer cells (HepG2, MDA-MB-231) and normal cells (HBL-100) with IC₅₀ values of 5.0 μM, 3.9 μM and ＞100 μM, respectively^[1].
Anticancer agent 84 displays good c-MYC G4 binding and stabilization abilities^[1].
Anticancer agent 84 blocks c-MYC transcription by targeting the promoter G4, leading to c-MYC-dependent cancer cell death in triple-negative breast cancer cell MDA-MB-23^[1].
Anticancer agent 84 (2 μM) significantly disrupts the binding of the three proteins (NM23-H2, BLM and DHX36) to c-MYC G4 with IC₅₀ values of 0.16 μM, 2.3 μM and 7.0 μM, respectively^[1].
Anticancer agent 84 (0-5 μM) impacts c-MYC-related events in TNBC, including proliferation, invasion, cell cycle, and apoptosis^[1].

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

Western Blot Analysis^[1]

Cell Line:	MDA-MB-231 cells
Concentration:	1.25, 2.5, 5 μM
Incubation Time:	48 h
Result:	Decreased the mRNA levels of c-MYC.

Cell Cycle Analysis^[1]

Cell Line:	MDA-MB-231 cells
Concentration:	1.25, 2.5, 5 μM
Incubation Time:	24 h
Result:	Could arrest MDA-MB-231 cells at the Sub G0 phase.

Apoptosis Analysis^[1]

Cell Line:	MDA-MB-231 cells
Concentration:	1.25, 2.5, 5 μM
Incubation Time:	24 h
Result:	Induced early apoptosis and necrosis in MDA-MB-231 cells.

RT-PCR^[1]

Cell Line:	MDA-MB-231 cells
Concentration:	1.25, 2.5 μM
Incubation Time:	24 h
Result:	Exhibited relatively weak effects on other genes and suppressed c-MYC transcription by targeting c-MYC G4.

Cell Cytotoxicity Assay^[1]

Cell Line:	MDA-MB-231 cells
Concentration:
Incubation Time:	48 h
Result:	Displayed good cytotoxicity against various cancer cells, including MDA-MB-231, MCF-7, HepG2, and SiHa and displayed less cytotoxicity against normal HBL-100 and NCM460 cells.

Cell Proliferation Assay^[1]

Cell Line:	MDA-MB-231 cells
Concentration:	1.25, 2.5, 5 μM
Incubation Time:	10 days
Result:	Exhibits good antiproliferative activity.

Cell Invasion Assay^[1]

Cell Line:	MDA-MB-231 cells
Concentration:	1.25, 2.5, 5 μM
Incubation Time:	24 h
Result:	Obviously decreased the invasion with an IC₅₀ value of 1.7 μM.

In Vivo

Anticancer agent 84 (i.p.; 2.5 mg/kg; daily; for 24 days) significantly inhibits tumor growth in the MDAMB-231 mouse xenograft model accompanied by c-MYC downregulation^[1].

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

Animal Model:	BALB/C-nu/nu mice(female, five-week-aged, 10−12 g)^[1]
Dosage:	2.5 mg/kg
Administration:	intraperitoneally, daily, for 24 days
Result:	Exhibited potent antitumor activity and could act as a c-MYC repressor in vivo.

Molecular Weight

994.18

Formula

C₅₇H₆₇N₇O₉

CAS No.

2714510-72-0

SMILES

CCN1C2=CC=C(C=C2C3=C1C=CC=C3)C4=NC(C5=CC=C(C=C5)N6CCN(CC6)C)=C(N4C7=CC=C(C=C7)OCCOCCOC8(O[C@@H]9O[C@H]([C@@H]([C@H]([C@@H]9O8)O)O)CO)C)C%10=CC=C(C=C%10)N%11CCN(CC%11)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]. Mao-Lin Li, et al. Design, Synthesis, and Evaluation of New Sugar-Substituted Imidazole Derivatives as Selective c-MYC Transcription Repressors Targeting the Promoter G-Quadruplex. J Med Chem. 2022 Sep 19. [Content Brief]