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

Karenitecin (Synonyms: Cositecan; BNP 1350)

製品番号: HY-14812 純度: 98.30%
取扱説明書

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

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Karenitecin 構造式

Karenitecin 構造式

CAS 番号 : 203923-89-1

容量 価格(税別) 在庫状況 数量
10 mM * 1  mL in DMSO USD 605 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 550 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 850 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 1750 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 2750 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 4200 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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製品説明

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

IC50 & Target[1]

Topoisomerase I

 

体外実験

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].

体内実験

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].

臨床実験
分子量

448.59

分子式

C₂₅H₂₈N₂O₄Si

CAS 番号

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
参考文献
細胞実験

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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献
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Keywords:

KarenitecinCositecanBNP 1350BNP1350BNP-1350TopoisomeraseInhibitorinhibitorinhibit

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製品名:
Karenitecin
製品番号:
HY-14812
数量:
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