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E[c(RGDfK)]2 (SU 016), c(RGDfK)的二聚体形式,与单体相比,显示出改进的肿瘤靶向性。E[c(RGDfK)]2可以很容易地与染料、药物分子或螯合剂偶联。
编号:175196
CAS号:250612-47-6
单字母:Glu[c(RGDfK)]-c(RGDfK)
编号: | 175196 |
中文名称: | 双c(RGD)环肽:E[c(RGDfK)]2、Glu[cyclo(RGDfK)]-cyclo(RGDfK) |
英文名: | Glu[cyclo(RGDfK)]-cyclo(RGDfK) |
英文同义词: | E[c(RGDfK)]-c(RGDfK) |
CAS号: | 250612-47-6 |
单字母: | Glu[c(RGDfK)]-c(RGDfK) |
三字母: | Glu(cyclo(Arg-Gly-Asp-DPhe-Lys))-cyclo(Arg-Gly-Asp-DPhe-Lys) |
氨基酸个数: | 11 |
分子式: | C₅₉H₈₇N₁₉O₁₆ |
平均分子量: | 1318.46 |
外观与性状: | 白色粉末状固体 |
来源: | 人工化学合成,仅限科学研究使用,不得用于人体。 |
纯度: | 95%、98% |
盐体系: | 可选TFA、HAc、HCl或其它 |
生成周期: | 2-3周 |
修饰类型: | 酰胺键成环 |
储存条件: | 负80℃至负20℃ |
标签: | RGD、RAD肽 |
E[c(RGDfK)]2 (SU 016), c(RGDfK)的二聚体形式,与单体相比,显示出改进的肿瘤靶向性。E[c(RGDfK)]2可以很容易地与染料、药物分子或螯合剂偶联。这个⁶⁸DOTA-E的Ga络合物(c(RGDfK))₂ 已被评估为治疗放射性药物。
E(c(RGDfK))₂ (SU 016), a dimeric form of c(RGDfK), showed improved tumor targeting properties compared to the monomer. E(c(RGDfK))₂ can be easily conjugated to dyes, drug molecules, or chelators. The ⁶⁸Ga complex of DOTA-E(c(RGDfK))₂ has been evaluated as theranostic radiopharmaceutical
H-GluCyclo(Arg-Gly-Asp-D-Phe-Lys)2 is a peptide macrocycle that is a biologically active peptide. The peptide was synthesized using the Fmoc/tBu strategy on Rink amide resin and deprotected with trifluoroacetic acid. H-GluCyclo(Arg-Gly-Asp-D-Phe-Lys)2 has been shown to have tumor necrosis factor antagonist activity, as well as inhibitory effects on integrins. It also inhibits the proliferation of cancer cells in vitro and in vivo. This peptide binds to the integrin alpha3beta1, which is expressed at high levels on many types of cancer cells, including prostate cancer cells.
H-GluCyclo(Arg-Gly-Asp-D-Phe-Lys)2 is a peptide that is used as a targeting agent for tumor imaging. It has been shown to be an effective imaging agent for tumors by binding to the RGD sequence in the extracellular matrix of the tumor. This peptide can be derivatized with fluorochromes and other functional groups for use as a contrast agent or as a labeling reagent. H-GluCyclo(Arg-Gly-Asp-D-Phe-Lys)2 has also been shown to inhibit angiogenesis and induce apoptosis, which may be due to its ability to bind to integrin receptors on endothelial cells and block their proliferation.
RGD肽-说明
RGD肽是指含有由Arg-Gly-Asp三个氨基酸组成的序列多肽,有直线肽和环肽之分。它们是许多细胞外基质蛋白(如VN、FN、FGN、胶原等)等最小识别短肽序列。
研究发现,RGD序列肽具有广泛的生物活性,可用于心血管疾病、骨质疏松和炎症等疾病的治疗,还可以预防和治疗由细胞粘附异常而导致的肿瘤,尤其是发展性肿瘤的转移;另一方面,RGD 序列肽又可作为兴奋剂,促进损伤的器官与组织的再生、伤口的愈合等等,RGD作为某些整合素的受体,其选择性部分依赖于RGD的构象以及RGD周围的氨基酸残基。
为此,近几年,许多科技工作者合成了一系列RGD三肽、四肽、五肽等,还合成了RGD环肽、双线肽、RGD模拟肽等等。为了满足客户对各种RGD序列肽的需求,专肽生物提供最广泛的RGD序列肽库,以满足科研工作者对RGD肽的需求。
专肽生物提供各种RGD肽的现货,缩短科研工作者的项目时间,例如c(RGDfK)、c(RGDfC)、c(RADyK)、c(RGDyK)、c(RADfC)、环状多肽c(RGDfK)-巯基乙酸、c(RGDfK)-PEG2-巯基乙酸、Mpa-Ahx-c(RGDfK)、环状多肽c(RGDfK)-半胱氨酸、DOTA-c(RGDfK)、NOTA-c(RGDfK)、NOTA-c(RGDyK)、DOTA-c(RGDyK)、E[c(RGDfK)]2、E[c(RGDyK)]2、DDDDD-c(RGDfK)等等,具体可咨询销售人员。
DOI | 名称 | |
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10.1016/j.nucmedbio.2013.01.003 | Design and biological evaluation of ⁹⁹mTc-N₂S₂-Tat(49-57)-c(RGDyK): a hybrid radiopharmaceutical for tumors expressing α(v)β(3) integrins | 下载 |
10.1002/jbm.a.31615 | Arg-Gly-Asp (RGD) peptide conjugated poly(lactic acid)-poly(ethylene oxide) micelle for targeted drug delivery | 下载 |
10.1016/j.ijpharm.2008.09.055 | In vitro and in vivo evaluation of a paclitaxel conjugate with the divalent peptide E-[c(RGDfK)2] that targets integrin alpha v beta 3 | 下载 |
10.1016/j.nucmedbio.2014.09.010 | Preparation and preclinical evaluation of (66)Ga-DOTA-E(c(RGDfK))2 as a potential theranostic radiopharmaceutical | 下载 |