2. Apoptosis
  3. Apoptosis
  4. Antitumor agent-61

Antitumor agent-61 (Compound 9b), Irinotecan (Ir) derivative, is a potential antitumor agent. Antitumor agent-61 displays potent activity with IC50s of 0.92, 1.39, 1.75, 2.20, 3.05 and 3.23 μM against five human cancer cells SK-OV-3, SK-OV-3/CDDP, U2OS, MCF-7, A549 and MG-63, respectively. Antitumor agent-61 induces SK-OV-3 cells apoptosis through mitochondrion pathways.

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Antitumor agent-61 Chemical Structure

Antitumor agent-61 Chemical Structure

CAS No. : 2408917-12-2

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Antitumor agent-61 Related Antibodies

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Description

Antitumor agent-61 (Compound 9b), Irinotecan (Ir) derivative, is a potential antitumor agent. Antitumor agent-61 displays potent activity with IC50s of 0.92, 1.39, 1.75, 2.20, 3.05 and 3.23 μM against five human cancer cells SK-OV-3, SK-OV-3/CDDP, U2OS, MCF-7, A549 and MG-63, respectively. Antitumor agent-61 induces SK-OV-3 cells apoptosis through mitochondrion pathways[1].

In Vitro

Antitumor agent-61 (compound 6b) shows anti-proliferation activity with IC50 values of 3.05, 2.20, 3.23, 1.75, 0.92 and 1.39 μM for A549, MCF-7, MG-63, U2OS, SK-OV-3 and SK-OV-3/CDDP cells[1].
Antitumor agent-61 (compound 6b) (50-150 μM) shows a certain inhibitory activity against Topo I at 150 μM[1].
Antitumor agent-61 (compound 6b) (5-10 μM; 24 hours, SK-OV-3 cells) induces apoptosis through mitochondrial pathway. Decrease the MMP level and increase ROS level in a dose-dependent manner [1].

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

Antitumor agent-61 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: SK-OV-3 cells
Concentration: 5.0 and 10 μM
Incubation Time: 24 hours
Result: Increased the percentage of apoptosis cells (including the early and late apoptosis) from 21.11% (5 μM) to 32.27% (10 μM), respectively and the apoptosis rate was significantly greater than that of Ir.

Cell Cycle Analysis[1]

Cell Line: SK-OV-3 cells
Concentration: 5.0 and 10 μM
Incubation Time: 24 hours
Result: Increased the percentage of S stage in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: SK-OV-3 cells
Concentration: 5.0 and 10 μM
Incubation Time: 24 hours
Result: Decreased the expression of antiapoptotic protein Bcl-2, while increased pro-apoptotic Bax and caspase expression.
In Vivo

Antitumor agent-61 (compound 6b) (10-20 mg/kg; i.h.; Twice daily, for 28 days; BALB/c nude mice with SK-OV-3 xenograft) reduces mean NPC tumor burden in a dose-dependent manner[1].

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

Animal Model: BALB/c nude mice with SK-OV-3 xenograft[1]
Dosage: 10 and 20 mg/kg
Administration: Subcutaneous injection; Twice daily, for 28 days.
Result: Suppressed tumor growth by 47.7% and 56.8% for 10 and 20 mg/kg, respectively, without affecting body weight or causing any overt adverse effects.
Molecular Weight

992.08

Formula

C54H63FN5O10P
CAS No.
SMILES

O=C(N1CCC(CC1)N2CCCCC2)OC3=CC4=C(CC)C5=C(C6=CC7=C(COC(C7(CC)OC(CCCC8=CC=C(NC(P(OCC)(OCC)=O)C9=CC=C(C=C9)F)C=C8)=O)=O)C(N6C5)=O)N=C4C=C3
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Antitumor agent-61 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-612408917-12-2Antitumor agent61Antitumor agent 61ApoptosisIrinotecanIr derivativeantitumor agentSK-OV-3SK-OV-3/CDDPU2OSMCF-7A549 MG-63apoptosismitochondrion pathwayInhibitorinhibitorinhibit

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