EC0489是叶酸和去乙酰长春碱酰肼的偶联物，是叶酸受体(FR)的高亲和力配体。有望治疗难治性或转移性肿瘤。是一种小分子-药物偶联物(SMDC)。
货号:ajcx12796
CAS:1096702-14-5
分子式:C111H156N22O43S2
分子量：2550.68
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

[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.