| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C54H63FN5O10P |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Antitumor agent-61 is an Irinotecan (Ir) derivative and a potential antitumor agent. It shows potent activity, with IC50 values of 0.92, 1.39, 1.75, 2.20, 3.05, and 3.23 μM against the human cancer cell lines SK-OV-3, SK-OV-3/CDDP, U2OS, MCF-7, A549, and MG-63, respectively, and it induces apoptosis in SK-OV-3 cells through mitochondrial pathways[1]. It has a molecular formula of C54H63FN5O10P and a molecular weight of 992.08 g/mol.
Physical & Chemical Properties
| CAS Number | 2408917-12-2 |
|---|---|
| Molecular Formula | C54H63FN5O10P |
| Molecular Weight | 992.08 g/mol |
| 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 |
| Signaling Pathway | Apoptosis |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
Antitumor agent-61 exhibits anti-proliferative activity, with IC50 values of 3.05 μM (A549), 2.20 μM (MCF-7), 3.23 μM (MG-63), 1.75 μM (U2OS), 0.92 μM (SK-OV-3), and 1.39 μM (SK-OV-3/CDDP)[1]. Antitumor agent-61 shows a certain inhibitory activity against Topo I at 150 μM (50-150 μM)[1]. In SK-OV-3 cells, Antitumor agent-61 (5-10 μM; 24 hours) induces apoptosis through the mitochondrial pathway, decreasing MMP level and increasing ROS level in a dose-dependent manner[1].
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
In BALB/c nude mice bearing SK-OV-3 xenografts, Antitumor agent-61 given at 10-20 mg/kg (i.h.; twice daily for 28 days) lowers mean NPC tumor burden dose-dependently[1].
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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