EC0489

Modify Date: 2025-08-25 10:44:42

EC0489 Structure
EC0489 structure
Common Name EC0489
CAS Number 1096702-14-5 Molecular Weight 2550.68
Density N/A Boiling Point N/A
Molecular Formula C111H156N22O43S2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of EC0489


EC0489, a conjugate of folic acid and desacetyl vinblastine hydrazide, is a high-affinity ligand for the folate receptor (FR). Refractory or metastatic Tumor[1]. Small molecule-drug conjugate (SMDC)[2].

 Names

Name EC0489

 EC0489 Biological Activity

Description EC0489, a conjugate of folic acid and desacetyl vinblastine hydrazide, is a high-affinity ligand for the folate receptor (FR). Refractory or metastatic Tumor[1]. Small molecule-drug conjugate (SMDC)[2].
Related Catalog
Target

Folate receptor[1]

In Vitro The affinity of EC0489 toward the folate receptor (FR) is approximately half of that of folic acid (relative affinity 0.50)[1]. FR-positive KB cells are highly sensitive to EC0489 with an IC50 of 5 nM[1].
In Vivo EC0489 has a favorable toxicology profile in Rats. EC0489 (2, 3, and 4 μmol/kg) has antitumor activity against mice KB tumor models in a dose-dependent manner[1].
References

[1]. Leamon CP, et al. Reducing undesirable hepatic clearance of a tumor-targeted vinca alkaloid via novel saccharopeptidic modifications. J Pharmacol Exp Ther. 2011 Feb;336(2):336-43.

[2]. Zhuang C, et al. Small molecule-drug conjugates: A novel strategy for cancer-targeted treatment. Eur J Med Chem. 2019 Feb 1;163:883-895.

 Chemical & Physical Properties

Molecular Formula C111H156N22O43S2
Molecular Weight 2550.68
InChIKey PHCAWPRQWLBYTH-HCDHKMFTSA-N
SMILES CCC1(O)CC2CN(CCc3c([nH]c4ccccc34)C(C(=O)OC)(c3cc4c(cc3OC)N(C)C3C(O)(C(=O)NNC(=O)OCCSSCC(NC(=O)C(CCC(=O)NCC(O)C(O)C(O)C(O)CO)NC(=O)C(CCC(=O)O)NC(=O)C(CCC(=O)NCC(O)C(O)C(O)C(O)CO)NC(=O)C(CCC(=O)O)NC(=O)C(CCC(=O)NCC(O)C(O)C(O)C(O)CO)NC(=O)CCC(NC(=O)c5ccc(NCc6c[nH]c7nc(N)nc(=O)c-7n6)cc5)C(=O)O)C(=O)O)C(O)C5(CC)C=CCN6CCC43C65)C2)C1
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