Edotecarin (Synonyms: J 107088; PF 804950)

Cat. No.: HY-13618: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

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.

Edotecarin Chemical Structure

CAS No. : 174402-32-5

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Topoisomerase Topo I Topo II

Biological Activity
Purity & Documentation
References
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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)

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	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/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

Molecular Weight

608.55

Formula

C₂₉H₂₈N₄O₁₁

CAS No.

174402-32-5

Appearance

Solid

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

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

Purity: 98.39%

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Data Sheet (278 KB) SDS (251 KB)

COA (263 KB) HNMR (222 KB) RP-HPLC (299 KB) LCMS (265 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]

Edotecarin Related Classifications

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Edotecarin174402-32-5J 107088 PF 804950J107088J-107088PF804950PF 804950PF-804950TopoisomeraseInhibitorinhibitorinhibit

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