Antitumor agent-138

Name: Antitumor agent-138
Brand: MedChemExpress
SKU: HY-162227

Cat. No.: HY-162227: Ficha de datos Instrucciones de manejo
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Antitumor agent-138 (compound 5b) is an inhibitor against tubulin polymerization at tubulin colchicine-binding sites, with IC₅₀ of 1.87 μM. Antitumor agent-138 arrests the cell cycle at G2/M phase and induces an apoptosis in MCF-7 cells. Antitumor agent-138 inhibits cells migration and angiogenesis.

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Antitumor agent-138 Estructura química

No. CAS : 2975168-22-8

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Descripciòn

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.39 μM Compound: 5b	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 38280356]
HeLa	IC₅₀	0.11 μM Compound: 5b	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 38280356]
HT-29	IC₅₀	0.06 μM Compound: 5b	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 38280356]
L02	IC₅₀	2.73 μM Compound: 5b	Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 38280356]
MCF7	IC₅₀	0.04 μM Compound: 5b	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 38280356]
MDA-MB-231	IC₅₀	0.04 μM Compound: 5b	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 38280356]

In Vitro

Antitumor agent-138 exhibits anti-proliferative properties in cells MCF-7, A549, MDA-MB-231, HT-29, HeLa and L02, with IC₅₀s of 0.04, 0.39, 0.04, 0.06, 0.11 and 2.73 μM, respectively^[1].
Antitumor agent-138 (5-20 nM) inhibits the colony formation in human breast cancer cells MCF-7^[1].
Antitumor agent-138 (25-200 nM) induces microtubule collapse in MCF-7 cellls^[1].
Antitumor agent-138 (6.25-50 nM) inhibits the HUVEC tubes formation in a dose-dependent manner and exhibits an anti-vascular activity^[1].

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

Cell Migration Assay ^[1]

Cell Line:	A549
Concentration:	6.25-50 nM
Incubation Time:	24 h
Result:	Inhibited the cell migration in a dose-dependent manner.

Cell Proliferation Assay^[1]

Cell Line:	MCF-7, A549, MDA-MB-231, HT-29, HeLa and L02
Concentration:	0-5 μM
Incubation Time:	48 h
Result:	Exhibited anti-proliferative properties in cancer cells MCF-7, A549, MDA-MB-231, HT-29, HeLa with low concentrations in nanomole.

Western Blot Analysis^[1]

Cell Line:	MCF-7
Concentration:	6.25-25 nM
Incubation Time:	24 h
Result:	Increased P21, Cyclin B1, Cdc25c and cdk7 in a dose- and time-dependent manner. Increased Bax, Cleaved-PARP, Bim and Cleaved Caspase-9, decreasesd Bcl-2 in a dose- and time-dependent manner.

Immunofluorescence^[1]

Cell Line:	MCF-7
Concentration:	25-200 nM
Incubation Time:	8 h
Result:	Disrupted the microtubule network into punctate.

In Vivo

Antitumor agent-138 (20 mg/kg, i.p., 21 days) exhibits an antitumor activity with a tumor growth inhibition rate of 68.95% in MCF-7 xenograft BALB/c nude mice^[1].

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

Animal Model:	MCF-7 xenograft in BALB/c nude mice^[1]
Dosage:	20 mg/kg
Administration:	intraperitoneal injection for 21 days
Result:	Inhibited the tumor growth with TGI of 68.95%

Peso molecular

367.40

Fòrmula

C₂₀H₂₁N₃O₄

No. CAS

2975168-22-8

SMILES

CC1=CC=C(C2=CC(N)=NN2C(C3=CC(OC)=C(OC)C(OC)=C3)=O)C=C1

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Yang Y, et al., Design and synthesis of novel 3-amino-5-phenylpyrazole derivatives as tubulin polymerization inhibitors targeting the colchicine-binding site. Eur J Med Chem. 2024 Jan 24;267:116177. [Content Brief]