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Cat. No.: HY-13618

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Edotecarin

(Synonyms: J 107088; PF 804950)

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.

CAS No.: 174402-32-5
Formula: C₂₉H₂₈N₄O₁₁
Molecular Weight:608.55

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Edotecarin Chemical Structure

CAS No.: 174402-32-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Edotecarin is a potent inhibitor of topoisomerase I that can induces single-strand DNA cleavage, with IC₅₀ of 50 nM.

IC₅₀ & Target^[1]

Topoisomerase I

50 nM (IC₅₀)

Protein Kinase C

160 μM (IC₅₀)

All Topoisomerase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	6.5 nM Compound: Edotecarin	Cytotoxicity against human A2780 cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human A2780 cells after 72 hrs by sulforhodamine B assay	[PMID: 22749423]
DLD-1	IC₅₀	840 nM Compound: 1	Cytotoxicity against human DLD1 cells after 72 hrs Cytotoxicity against human DLD1 cells after 72 hrs	[PMID: 19397324]
GLC4 cell line	IC₅₀	0.8 nM Compound: Edotecarin	Cytotoxicity against human GLC4 cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human GLC4 cells after 72 hrs by sulforhodamine B assay	[PMID: 22749423]
MKN-45	IC₅₀	4.8 nM Compound: 2	Tested for cytotoxic activity against human stomach cancer cells (MKN-45) Tested for cytotoxic activity against human stomach cancer cells (MKN-45)	[PMID: 10743939]
MKN-45	IC₅₀	70 nM Compound: 1	Cytotoxicity against human MKN45 cells after 72 hrs Cytotoxicity against human MKN45 cells after 72 hrs	[PMID: 19397324]
NCI-H460	IC₅₀	193 nM Compound: Edotecarin	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	[PMID: 22749423]
P388	IC₅₀	1.5 nM Compound: 2	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)	[PMID: 10743939]
P388/S	EC₅₀	1.5 nM Compound: 1	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	[PMID: 19397324]
P388/S	IC₅₀	4.8 nM Compound: 1	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	[PMID: 19397324]

In Vitro

In the presence of human colon cancer cells labeled with ³Hthymidine, edotecarin (0.6 μmol/L) increases the formation of DNA-protein complexes in a time-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Edotecarin produces an 83% increase in survival in mice bearing intracranial D-456MG glioma and shows a strong antimetastatic effect^[1]. Edotecarin results in tumor growth delays ranging from 10.45 days at the lowest dose (3 mg/kg) to 24.83 days at the highest (100 mg/kg). Combination treatment of edotecarin plus irinotecan improves antitumor activity in vivo compared with either agent alone^[2].

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 A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 174402-32-5
Appearance Solid
Molecular Weight 608.55
Formula C₂₉H₂₈N₄O₁₁
Color Yellow to orange
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
Synonyms

J 107088; PF 804950
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Purity & Documentation
References

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Edotecarin

High-Throughput Bioactive Compound Library

All Topoisomerase Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Edotecarin Related Classifications

HY-13618 Related Classifications