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1096702-14-5

1096702-14-5 Structure

1096702-14-5 Structure
IdentificationBack Directory
[Name]

EC0489
[CAS]

1096702-14-5
[Synonyms]

EC0489
[Molecular Formula]

C111H156N22O43S2
[MDL Number]

MFCD31807644
[MOL File]

1096702-14-5.mol
[Molecular Weight]

2550.7
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

Soluble in DMSO
Hazard InformationBack Directory
[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].

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].

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.

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