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 Chemical Structure

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].

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
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Purity & Documentation
References
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Antitumor agent-138 Related Classifications

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  • 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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