Edotecarin
Based on 1 Customer Validation
Edotecarin is a potent inhibitor of topoisomerase I that can induces single-strand DNA cleavage, with IC50 of 50 nM.
For research use only. We do not sell to patients.
- Purity: 99.91%
- CAS No.: 174402-32-5
- Formula: C29H28N4O11
- Molecular Weight:608.55
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Belotecan hydrochloride
All Topoisomerase Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
Topoisomerase I 50 nM (IC50) |
Protein Kinase C 160 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
6.5 nM
Compound: Edotecarin
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Cytotoxicity against human A2780 cells after 72 hrs by sulforhodamine B assay
Cytotoxicity against human A2780 cells after 72 hrs by sulforhodamine B assay
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[PMID: 22749423] |
| DLD-1 | IC50 |
840 nM
Compound: 1
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Cytotoxicity against human DLD1 cells after 72 hrs
Cytotoxicity against human DLD1 cells after 72 hrs
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[PMID: 19397324] |
| GLC4 cell line | IC50 |
0.8 nM
Compound: Edotecarin
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Cytotoxicity against human GLC4 cells after 72 hrs by sulforhodamine B assay
Cytotoxicity against human GLC4 cells after 72 hrs by sulforhodamine B assay
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[PMID: 22749423] |
| MKN-45 | IC50 |
4.8 nM
Compound: 2
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Tested for cytotoxic activity against human stomach cancer cells (MKN-45)
Tested for cytotoxic activity against human stomach cancer cells (MKN-45)
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[PMID: 10743939] |
| MKN-45 | IC50 |
70 nM
Compound: 1
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Cytotoxicity against human MKN45 cells after 72 hrs
Cytotoxicity against human MKN45 cells after 72 hrs
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[PMID: 19397324] |
| NCI-H460 | IC50 |
193 nM
Compound: Edotecarin
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Cytotoxicity against human NCI-H460 cells after 72 hrs by sulforhodamine B assay
Cytotoxicity against human NCI-H460 cells after 72 hrs by sulforhodamine B assay
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[PMID: 22749423] |
| P388 | IC50 |
1.5 nM
Compound: 2
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The compound was tested for the cytotoxic activity against murine leukemia cells (P388)
The compound was tested for the cytotoxic activity against murine leukemia cells (P388)
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[PMID: 10743939] |
| P388/S | EC50 |
1.5 nM
Compound: 1
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Inhibition of DNA topoisomerase 1 in mouse P388/S cells assessed as formation of topoisomerase 1-DNA complex by proteinase K/SDS method
Inhibition of DNA topoisomerase 1 in mouse P388/S cells assessed as formation of topoisomerase 1-DNA complex by proteinase K/SDS method
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[PMID: 19397324] |
| P388/S | IC50 |
4.8 nM
Compound: 1
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Cytotoxicity against mouse P388/S cells after 72 hrs by colorimetric tetrazolium-formazan method
Cytotoxicity against mouse P388/S cells after 72 hrs by colorimetric tetrazolium-formazan method
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[PMID: 19397324] |
In Vitro
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 174402-32-5
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Appearance Solid
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Molecular Weight 608.55
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Formula C29H28N4O11
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Color Yellow to orange
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SMILES
O=C1N(NC(CO)CO)C(C2=C1C3=C(C4=C2C5=C(N4[C@H]6[C@@H]([C@H]([C@@H]([C@@H](CO)O6)O)O)O)C=C(O)C=C5)NC7=C3C=CC(O)=C7)=O
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Synonyms
J 107088; PF 804950
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (164.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Saif MW, et al. Edotecarin: a novel topoisomerase I inhibitor. Clin Colorectal Cancer. 2005 May;5(1):27-36. [Content Brief]
[2]. Ciomei M, et al. Antitumor efficacy of edotecarin as a single agent and in combination with chemotherapy agents in a xenograft model. Clin Cancer Res. 2006 May 1;12(9):2856-61. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6433 mL | 8.2163 mL | 16.4325 mL | 41.0813 mL |
| 5 mM | 0.3287 mL | 1.6433 mL | 3.2865 mL | 8.2163 mL | |
| 10 mM | 0.1643 mL | 0.8216 mL | 1.6433 mL | 4.1081 mL | |
| 15 mM | 0.1096 mL | 0.5478 mL | 1.0955 mL | 2.7388 mL | |
| 20 mM | 0.0822 mL | 0.4108 mL | 0.8216 mL | 2.0541 mL | |
| 25 mM | 0.0657 mL | 0.3287 mL | 0.6573 mL | 1.6433 mL | |
| 30 mM | 0.0548 mL | 0.2739 mL | 0.5478 mL | 1.3694 mL | |
| 40 mM | 0.0411 mL | 0.2054 mL | 0.4108 mL | 1.0270 mL | |
| 50 mM | 0.0329 mL | 0.1643 mL | 0.3287 mL | 0.8216 mL | |
| 60 mM | 0.0274 mL | 0.1369 mL | 0.2739 mL | 0.6847 mL | |
| 80 mM | 0.0205 mL | 0.1027 mL | 0.2054 mL | 0.5135 mL | |
| 100 mM | 0.0164 mL | 0.0822 mL | 0.1643 mL | 0.4108 mL |
Edotecarin Related Classifications
HY-13618 Related Classifications
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