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ChemicalBook >> CAS DataBase List >>EC0489

EC0489

CAS No.
1096702-14-5
Chemical Name:
EC0489
Synonyms
EC0489;Vincaleukoblastin-23-oic acid, O4-deacetyl-, 2-[(2-mercaptoethoxy)carbonyl]hydrazide, disulfide with N-[4-[[(2-amino-3,4-dihydro-4-oxo-6-pteridinyl)methyl]amino]benzoyl]-L-γ-glutamyl-N-(1-deoxy-D-glucitol-1-yl)-L-glutaminyl-L-α-glutamyl-N-(1-deoxy-D-glucitol-1-yl)-L-glutaminyl-L-α-glutamyl-N-(1-deox...
CBNumber:
CB84844745
Molecular Formula:
C111H156N22O43S2
Molecular Weight:
2550.7
MDL Number:
MFCD31807644
MOL File:
1096702-14-5.mol
Last updated:2023-05-21 10:59:17

EC0489 Properties

Density 1.66±0.1 g/cm3(Predicted)
storage temp. Store at -20°C
solubility Soluble in DMSO

EC0489 Chemical Properties,Uses,Production

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.

EC0489 Preparation Products And Raw materials

Raw materials

Preparation Products

EC0489 Suppliers

Global( 3)Suppliers
Supplier Tel Email Country ProdList Advantage
TargetMol Chemicals Inc. 		+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 32161 58
Fan De(Beijing) Biotechnology Co., Ltd. 15911056312 liming@bio-fount.com China 9729 58
DC Chemicals 021-58447131 13564518121 sales@dcchemicals.com China 9409 58
EC0489 Vincaleukoblastin-23-oic acid, O4-deacetyl-, 2-[(2-mercaptoethoxy)carbonyl]hydrazide, disulfide with N-[4-[[(2-amino-3,4-dihydro-4-oxo-6-pteridinyl)methyl]amino]benzoyl]-L-γ-glutamyl-N-(1-deoxy-D-glucitol-1-yl)-L-glutaminyl-L-α-glutamyl-N-(1-deoxy-D-glucitol-1-yl)-L-glutaminyl-L-α-glutamyl-N-(1-deox... 1096702-14-5