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

Karenitecin (Synonyms: Cositecan; BNP 1350)

Cat. No.: HY-14812 Purity: 98.30%
Handling Instructions

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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10 mM * 1 mL in DMSO USD 605 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 4200 In-stock
Estimated Time of Arrival: December 31
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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].

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].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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
Molecular Weight

448.59

Formula

C₂₅H₂₈N₂O₄Si

CAS No.

203923-89-1

SMILES

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

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Room temperature in continental US; may vary elsewhere

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Product Name:
Karenitecin
Cat. No.:
HY-14812
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Karenitecin

Cat. No.: HY-14812