2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. Antitumor agent-138

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

Antitumor agent-138 Chemical Structure

CAS No. : 2975168-22-8

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Antitumor agent-138 Related Antibodies

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Description

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[1].

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]
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]
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]
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.

Antitumor agent-138 Related Antibodies

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%
Molecular Weight

367.40

Formula

C20H21N3O4
CAS No.
SMILES

CC1=CC=C(C2=CC(N)=NN2C(C3=CC(OC)=C(OC)C(OC)=C3)=O)C=C1
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
References
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Antitumor agent-138 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Antitumor agent-1382975168-22-8Antitumor agent138Antitumor agent 138Microtubule/TubulinApoptosistubulin colchicine-binding sitesMCF-7 xenograftBALB/c nude miceMCF-7A549Inhibitorinhibitorinhibit

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