870295 | DSPE-RGD

1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[4-(p-(cysarginylglycylaspartate-maleimidomethyl)cyclohexane-carboxamide] (sodium salt)


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DSPE-RGD

DSPE-RGD

1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[4-(p-(cysarginylglycylaspartate-maleimidomethyl)cyclohexane-carboxamide] (sodium salt)

RGD modified liposomes show potential for cancer research
Hygroscopic
No
Light Sensitive
No
Molecular Formula
C68H120N9Na2O18PS
Percent Composition
C 55.91%, H 8.28%, N 8.63%, Na 3.15%, O 19.72%, P 2.12%, S 2.20%
Purity
>99%
Stability
1 Year
Storage Temperature
-20°C
Molecular Weight
1460.748
Exact Mass
1459.801
Synonyms
sodium (6S,12S,15R)-1-amino-6-ammonio-15-(((1-((4-((2-((((R)-2,3-bis(stearoyloxy)propoxy)oxidophosphoryl)oxy)ethyl)carbamoyl)cyclohexyl)methyl)-2,5-dioxopyrrolidin-3-yl)thio)methyl)-12-(carboxylatomethyl)-1-imino-7,10,13-trioxo-2,8,11,14-tetraazahexadecan-16-oate
Chen, C.W., D.W. Lu, M.K. Yeh, C.Y. Shiau, and C.H. Chiang. (2011). Novel RGD-lipid conjugate-modified liposomes for enhancing siRNA delivery in human retinal pigment epithelial cells. Int J Nanomedicine 6:2567-80. [PubMed] Cao, Y., Y. Zhou, Q. Zhuang, L. Cui, X. Xu, R. Xu, and X. He. (2015). Anti-tumor effect of RGD modified PTX loaded liposome on prostatic cancer. Int J Clin Exp Med 8:12182-91. [PubMed] Liposomes Modified with Cyclic RGD Peptide for Tumor Targeting Cyclic RGD peptide anchored sterically stabilized liposomes (RGD-SL) were investigated for selective and preferential presentation of carrier contents at angiogenic endothelial cells overexpressing alphavbeta3 integrins on and around tumor tissue and thus for assessing their targetabilty. Liposomes were prepared using distearoylphosphatidylcholine (DSPC), cholesterol and distearoylphosphatidylethanolamine-polyethyleneglycol-RGD peptide conjugate (DSPE-PEG-RGD) in a molar ratio 56:39:5. The control RAD peptide anchored sterically stabilized liposomes (RAD-SL) and liposome with 5 mol% PEG (SL) without peptide conjugate which had similar lipid composition were used for comparison. The average size of all liposome preparations prepared was approximately 105 nm and maximum drug entrapment was 10.5+/- 1.1%. In vitro endothelial cell binding of liposomes exhibited 7-fold higher binding of RGD-SL to HUVEC in comparison to the SL and RAD-SL. Spontaneous lung metastasis and angiogenesis assays show that RGD peptide anchored liposomes are significantly (p<0.01) effective in the prevention of lung metastasis and angiogenesis compared to free 5-FU, SL and RAD-SL. In therapeutic experiments, 5-FU, SL, RGD-SL and RAD-SL were administered intravenously on day 4 at the dose of 10 mg 5-FU/kg body weight to B16F10 tumor bearing BALB/c mice resulting in effective regression of tumors compared with free 5-FU, SL and RAD-SL. Results indicate that cyclic RGD peptide anchored sterically stabilized liposomes bearing 5-FU are significantly (p<0.01) active against primary tumor and metastasis than the non-targeted sterically stabilized liposomes and free drug. Thus cyclic RGD peptide anchored sterically stabilized liposomes hold potential of targeted cancer chemotherapeutics. Journal of Drug Targeting 12(5):257-64 June 2004