2. Cell Cycle/DNA Damage
  3. Topoisomerase
  4. Karenitecin

Karenitecin  (Synonyms: Cositecan; BNP 1350)

Cat. No.: HY-14812 Purity: 98.27%
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Karenitecin (Cositecan) is a topoisomerase I inhibitor, with potent anti-cancer activity.

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

Karenitecin Chemical Structure

Karenitecin Chemical Structure

CAS No. : 203923-89-1

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Based on 1 publication(s) in Google Scholar

Karenitecin Related Antibodies

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1 Publications Citing Use of MCE Karenitecin

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Topoisomerase Topo I Topo II

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

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Description

Karenitecin (Cositecan) is a topoisomerase I inhibitor, with potent anti-cancer activity.

IC50 & Target

Topoisomerase I

 

In Vitro

Karenitecin is a topoisomerase I inhibitor, with potent anti-cancer activity. Karenitecin inhibits cell growth of A253 cells with IC10, IC50, and IC90 values of 0.01, 0.07, and 0.7 μM after 2 h treatment. Karenitecin induces DNA damage (0.01, 0.07, and 0.7 μM), and increases cyclin E and cdk2 protein expression in A253 cells (0.07, and 0.7 μM). Karenitecin markedly enhances the cyclin B/cdc2-associated kinase activity at low concentration, but slightly suppresses this kinase activity at higher concentration[1]. Karenitecin inhibits several human colon cancer cell lines such as COLO205, COLO320, LS174T, SW1398 and WiDr cells, with IC50s of 2.4 nM, 1.5 nM, 1.6 nM, 2.9 nM, and 3.2 nM, respectively[2].

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

Karenitecin Related Antibodies
In Vivo

Karenitecin shows maximum growth inhibition of 61% on COLO320 cells and 54% on COLO205 colon cancer cells via i.p. administration of 1 mg/kg in mice. Karenitecin (1.0 mg/kg daily × 5 i.p.) significantly suppresses growth inhibition both in the parental Pgp-negative xenografts and in the Pgp-positive xenografts[2].

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

448.59

Formula

C25H28N2O4Si
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 3.03 mg/mL (6.75 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 2.2292 mL 11.1460 mL 22.2921 mL
5 mM 0.4458 mL 2.2292 mL 4.4584 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Cell Assay

sup>[1]Cell growth inhibition is determined using the total protein SRB assay as described elsewhere. Briefly, 600 cells/well are seeded onto 96-well plates. After 24 h, exponentially growing A253 cells are treated with Karenitecin, which is diluted in culture medium, for 2 h. At four doubling times after drug exposure, the cells are fixed with 10% trichloroacetic acid and further processed according to the published SRB procedure. The optical density is measured at 570 nm. Antiproliferative activities are expressed as drug concentrations that induce growth inhibition of 50 or 90% compared with growth of untreated controls (IC50 and IC90 values)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice[2]
The human tumor xenografts grown in nude mice are measured twice a week in 3 dimensions with vernier calipers. The volume is calculated by the equation length × width × thickness × 0.5, and expressed in mm3. At the start of treatment (designated as day 0), groups of 5 to 6 tumor-bearing mice are formed to provide a mean tumor volume of approximately 150 mm3 in each group. Doses of Karenitecin and CPT-11 for the daily × 5 schedule are administered according to the maximum tolerated dose (MTD) for tumor-bearing mice. This maximum tolerated dose is based on the occurrence of a mean weight loss of approximately 10% of the initial weight within the first 2 weeks after the start of the treatment. Recovery of the weight loss should be completed on day 14; consequently, mice are weighed on weekdays for 2 weeks and, thereafter, twice a week. The MTD is assessed in groups of 3 non-tumor-bearing nude mice per dose level[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2292 mL 11.1460 mL 22.2921 mL 55.7302 mL
5 mM 0.4458 mL 2.2292 mL 4.4584 mL 11.1460 mL
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Karenitecin 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:

Karenitecin203923-89-1Cositecan BNP 1350BNP1350BNP 1350BNP-1350TopoisomeraseInhibitorinhibitorinhibit

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