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

Belotecan  (Synonyms: CKD-602 free base)

Cat. No.: HY-13566 Purity: 99.40%
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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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Belotecan Related Antibodies

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1 Publications Citing Use of MCE Belotecan

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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.

Belotecan Related Antibodies

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.
Appearance

Solid

Color

Light yellow to yellow

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

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (28.84 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3068 mL 11.5340 mL 23.0681 mL
5 mM 0.4614 mL 2.3068 mL 4.6136 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.25 mg/mL (2.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3068 mL 11.5340 mL 23.0681 mL 57.6701 mL
5 mM 0.4614 mL 2.3068 mL 4.6136 mL 11.5340 mL
10 mM 0.2307 mL 1.1534 mL 2.3068 mL 5.7670 mL
15 mM 0.1538 mL 0.7689 mL 1.5379 mL 3.8447 mL
20 mM 0.1153 mL 0.5767 mL 1.1534 mL 2.8835 mL
25 mM 0.0923 mL 0.4614 mL 0.9227 mL 2.3068 mL
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Belotecan Related Classifications

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:

Belotecan256411-32-2CKD-602CKD602CKD 602TopoisomeraseApoptosisapoptosiscell-cycle arrestanti-tumorcancercamptotheciCaskiHeLaSiHaInhibitorinhibitorinhibit

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