(S)-10-Hydroxycamptothecin (Synonyms: ChEMBL 273862, NSC 107124) |
| Catalog No.GC10098 |
La (S)-10-hidroxicamptotecina (10-HCPT;10-hidroxicamptotecina) es un inhibidor de la topoisomerasa I del ADN aislado de la planta china Camptotheca accuminata. La (S)-10-hidroxicamptotecina muestra un notable efecto inductor de la apoptosis. La (S)-10-hidroxicamptotecina tiene potencial para el tratamiento de hepatoma, carcinoma gÁstrico, cÁncer de colon y leucemia.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 19685-09-7
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
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Cell lines |
Colo 205 cells |
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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]: | |
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Animal models |
BALB/c-nu mice with Colo 205 cells xenograft tumor |
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Dosage form |
Dissolved in propylene glycol; 1, 2.5, 5, 7.5 mg/kg per two or four days for 25days; oral administration |
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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. |
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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. |
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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. | |
| Cas No. | 19685-09-7 | SDF | |
| Sinónimos | ChEMBL 273862, NSC 107124 | ||
| 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[C@]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 | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7446 mL | 13.7231 mL | 27.4461 mL |
| 5 mM | 0.5489 mL | 2.7446 mL | 5.4892 mL |
| 10 mM | 0.2745 mL | 1.3723 mL | 2.7446 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)
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