1. Cell Cycle/DNA Damage Apoptosis
  2. Topoisomerase Apoptosis
  3. Belotecan

Belotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Belotecan hydrochloride) that retains the same biological activity.

For research use only. We do not sell to patients.

Belotecan Chemical Structure

Belotecan Chemical Structure

CAS No. : 256411-32-2

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Description

Belotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer[1].

IC50 & Target

IC50: 30 ng/mL (Caski cells), 150 ng/mL (HeLa cells), 150 ng/mL (SiHa cells)[1]

In Vitro

Belotecan (0-600 ng/mL; 0-72 h) time- and dose-dependently inhibits viability of Caski cells, HeLa cells and SiHa cells at 48 h with IC50 values of 30, 150 and 150 ng/mL, respectively[1].
Belotecan (0-150 ng/mL; 48 h) induces cell apoptosis and cell-cycle arrest, and affects PARP, cleaved PARP, BAX, p53, Ser15, cell cycle related protein expression and cancer invasion in cervical cancer[1].

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

Apoptosis Analysis[1]

Cell Line: Caski, HeLa and SiHa cell lines
Concentration: 0-150 ng/mL
Incubation Time: 48 h
Result: Showed strong pro-apoptotic activities to Caski, HeLa and SiHa cells.

Western Blot Analysis[1]

Cell Line: Caski, HeLa and SiHa cell lines
Concentration: 0-150 ng/mL
Incubation Time: 48 h
Result: Increased the expression of PARP, cleaved PARP, BAX, p53, Ser15, cyclin B1, phosphorylated cyclin B1 and phospho-cdc2 (Tyr15) protein, and decreased MMP2 and VEGF protein expression.

Cell Cycle Analysis[1]

Cell Line: Caski, HeLa and SiHa cell lines
Concentration: 0-150 ng/mL
Incubation Time: 48 h
Result: Induced cell-cycle arrest in the G2/M phase in cervical cancer.

Cell Invasion Assay[1]

Cell Line: Caski, HeLa and SiHa cell lines
Concentration: 0-150 ng/mL
Incubation Time: 48 h
Result: Inhibited cancer invasion in cervical cancer.
In Vivo

Belotecan (25 mg/kg; i.v. for 16 days at 4-day intervals) inhibits tumor growth in CaSki-xenografts nude mice[1].

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

Animal Model: BALB/c-nude mice with CaSki cells injection[1]
Dosage: 25 mg/kg
Administration: Intravenous injection; 25 mg/kg; 16 days at 4-day intervals
Result: Significantly inhibited the tumor growth and showed no significant difference in bodyweight of xenograft mice and the controls.
Clinical Trial
Molecular Weight

433.50

Formula

C25H27N3O4

CAS No.
SMILES

O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=C(CCNC(C)C)C5=CC=CC=C5N=C4C3=C2)=O

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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Belotecan 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.

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Belotecan
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HY-13566
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