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(S)-10-Hydroxycamptothecin inhibitor of topoisomerase I

Catalog No.B4745
Size Price Stock Qty
10mM (in 1mL DMSO)
$60.00
In stock
25mg
$40.00
In stock
100mg
$85.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

(S)-10-Hydroxycamptothecin

Biological Activity

Description 10-Hydroxycamptothecin is an inhibitor of DNA topoisomerase I with potent anti-tumor activity.
Targets DNA topoisomerase I          
IC50            

Protocol

Cell experiment [1]:

Cell lines

Colo 205 cells

Preparation method

Soluble in DMSO > 6.275mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

5, 10, 15, 20nM for 24, 48, 72, 96, 120hr

Applications

10-Hydroxycamptothecin inhibited the cell growth and reduced the cell viability of human colon cancer cell line Colo 205. The agent disturbed the cell cycle distribution which dramatically induced the increase of cell population in the G2/M phase and a decrease in the G0/G1 phase.

Animal experiment [2]:

Animal models

BALB/c-nu mice with Colo 205 cells xenograft tumor

Dosage form

Dissolved in propylene glycol; 1, 2.5, 5, 7.5 mg/kg per two or four days for 25days; oral administration

Application

The results of this study suggested that a relatively low dose of 10-Hydroxycamptothecin was able to inhibit the growth of colon cancer, with no acute toxicity observed.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Ping YH1, Lee HC, et al, Anticancer effects of low-dose 10-hydroxycamptothecin in human colon cancer. Oncol Rep. 2006 May;15(5):1273-9.

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Chemical Properties

Cas No. 19685-09-7 SDF Download SDF
Chemical Name (S)-4-ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
Canonical SMILES CC[[email protected]]1(O)C(C=C2C3=C(CN2C4=O)C=C5C=C(O)C=CC5=N3)=C4COC1=O
Formula C20H16N2O5 M.Wt 364.35
Solubility >23.8mg/mL in DMSO with gentle warming Storage Desiccate at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

IC50: 0.31 μM

10-Hydroxycamptothecin is a dose-dependent growth inhibitor of human microvascular endothelial cells (HMEC), and significantly inhibits the migration of HMEC with IC50 of 0.63 μM, resulting in a dose-dependent inhibition of tube formation with IC50 of 0.96 μM [1,2].

An antiangiogenic strategy may be effective as an anticancer therapy, because the growth and metastasis of solid tumors depend on the development of an adequate blood supply via angiogenesis [1,2].

In vitro: The proliferation of human microvascular endothelial cells (HMEC) and seven human tumor cell lines were detected by SRB assay, resulting in study the antiangiogenic potential of 10-hydroxycamptothecin (HCPT), ,and the endothelial cell migration and tube formation were assessed using two in vitro model systems[2].

In vivo: Using a modification of the chick embryo chorioallantoic membrane (CAM) assay defines inhibition of angiogenesis in vivo. Morphological assessment of apoptosis was performed by fluorescence microscope. HCPT 0.313-5 μmol/L treatment was in a dose-dependent inhibition of proliferation, migration and tube formation in HMEC cells, and HCPT 6.25-25 nmol/egg prevented angiogenesis in CAM assay. HCPT 1.25-5 μmol/L induced typical morphological changes of apoptosis (including condensed chromatin, nuclear fragmentation, and reduction in volume in HMEC cells). HCPT significantly blocked angiogenesis both in vitro and in vivo at relatively low concentrations, and this effect was connected with induction of apoptosis in HMEC cells. These results taken collectively reveal that HCPT may be a potential for antiangiogenetic and cytotoxic drug and further investigationis warranted [2,3].

Clinical trial: So far, no clinical study has been conducted.

References:
[1] Vladu B, Woynarowski JM, Manikumar G, Wani MC, Wall ME, Von Hoff DD, Wadkins RM.  7- and 10-substituted camptothecins: dependence of topoisomerase I-DNA cleavable complex formation and stability on the 7- and 10-substituents. Mol Pharmacol. 2000 Feb;57(2):243-51.
[2] Xiao D, Tan W, Li M, Ding J.  Antiangiogenic potential of 10-hydroxycamptothecin. Life Sci. 2001 Aug 24;69(14):1619-28.
[3] Ping YH, Lee HC, Lee JY, Wu PH, Ho LK, Chi CW, Lu MF, Wang JJ.  Anticancer effects of low-dose 10-hydroxycamptothecin in human colon cancer. Oncol Rep. 2006 May;15(5):1273-9.