EC0489

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

EC0489 

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。可用于难治性或转移性肿瘤的研究。 是一种小分子-药物偶联物 (SMDC)。

EC0489

EC0489 Chemical Structure

CAS No. : 1096702-14-5

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生物活性

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].

IC50 & Target

Folate receptor[1]

体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

2550.68

Formula

C111H156N22O43S2

CAS 号

1096702-14-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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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