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Cat. No.: HY-162227

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Antitumor agent-138

Name: Antitumor agent-138
Brand: MedChemExpress
SKU: HY-162227
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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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CAS No.: 2975168-22-8
Formule: C₂₀H₂₁N₃O₄
Masse moléculaire:367.40

Stockage:

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

Data Sheet (276 KB)

Antitumor agent-138 Chemical Structure

CAS No.: 2975168-22-8

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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%

Related Protocols :

Chemical Information

CAS No. 2975168-22-8
Masse moléculaire 367.40
Formule C₂₀H₂₁N₃O₄
SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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