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EC0489 Sale

目录号 : GC32401

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)。

EC0489 Chemical Structure

Cas No.:1096702-14-5

规格 价格 库存 购买数量
250mg 待询 待询
500mg 待询 待询

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Sample solution is provided at 25 µL, 10mM.

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产品描述

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.

Chemical Properties

Cas No. 1096702-14-5 SDF
Canonical SMILES [{Ggu}-QEQEQC]
分子式 C111H156N22O43S2 分子量 2550.68
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 0.3921 mL 1.9603 mL 3.9205 mL
5 mM 0.0784 mL 0.3921 mL 0.7841 mL
10 mM 0.0392 mL 0.196 mL 0.3921 mL
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Research Update

Reducing undesirable hepatic clearance of a tumor-targeted vinca alkaloid via novel saccharopeptidic modifications

J Pharmacol Exp Ther 2011 Feb;336(2):336-43.PMID:20978169DOI:10.1124/jpet.110.175109.

During a phase I trial of EC145 (a folate-targeted vinca alkaloid conjugate), constipation was identified as the dose-limiting toxicity, probably from a nonfolate receptor-related liver clearance process capable of releasing unconjugated vinca alkaloid from EC145 and shuttling it to the bile. Here, we report on the selective placement of novel carbohydrate segments (1-amino-1-deoxy-glucitolyl-γ-glutamate) spaced in-between the folate and vinca alkaloid moieties of EC145, which yielded a new agent (EC0489) that is equipotent but less toxic than EC145. Whereas both compounds could cure tumor-bearing mice reproducibly, EC0489 differed from EC145 with i) a shorter elimination half-life, ii) approximately 70% decrease in bile clearance, iii) a 4-fold increase in urinary excretion, and iv) improved tolerability in rodents. This combination of improvements justified the clinical evaluation of EC0489 where currently administered dose levels have exceeded the maximal tolerated dose of EC145 by approximately 70%, thereby reflecting the translational benefits to this new approach.