192948-77-9

PAMAM dendrimer G3.5 carboxylate (PAMAM G3.5) is a polyamidoamine (PAMAM) dendrimer with carboxylate termini that has been used as a drug delivery system in vitro and in vivo.1,2 It is approximately 66.1 Å in diameter in water and has 48 surface groups.3 PAMAM G3.5 is active against E. coli (IC50 = 22 mg/ml) and increases the mitochondrial membrane potential of isolated rat liver mitochondria when used at concentrations ranging from 10 to 50 µM.4,5 Unlike amine-terminated PAMAM G4.0, PAMAM G3.5 (20 µM) is not toxic to zebrafish embryos.6 A fluorescently labeled form of PAMAM G3.5 enters Caco-2 cells via dynamin-, clathrin-, and caveolin-mediated endocytosis.7 Conjugates of PAMAM G3.5 with the active fragment of the DNA cross-linking agent oxaliplatin (Item No. 13106) are cytotoxic to A2780 ovarian, MCF-7 breast, and Caco-2 colon cancer cells and BJ fibroblasts (IC50s = 0.08, 4.1, 0.39, and 3 µM, respectively).1 PAMAM G3.5 in complex with the topoisomerase I inhibitor camptothecin (Item No. 11694) increases the oral bioavailability of camptothecin in mice.2WARNING This product is not for human or veterinary use.

[1] CLÁUDIA CAMACHO J R Helena Tomás. Use of Half-Generation PAMAM Dendrimers (G0.5-G3.5) with Carboxylate End-Groups to Improve the DACHPtCl2 and 5-FU Efficacy as Anticancer Drugs.[J]. Molecules, 2021, 26 10. DOI: 10.3390/molecules26102924
[2] S. SADEKAR . Poly(amido amine) dendrimers as absorption enhancers for oral delivery of camptothecin[J]. International Journal of Pharmaceutics, 2013, 456 1: Pages 175-185. DOI: 10.1016/j.ijpharm.2013.07.071
[3] GABRIELLA CAMINATI  Donald A T  Nicholas J Turro. Photophysical investigation of starburst dendrimers and their interactions with anionic and cationic surfactants[J]. Journal of the American Chemical Society, 1990, 112 23: 8515-8522. DOI: 10.1021/ja00179a041
[4] BING WANG . Inhibition of bacterial growth and intramniotic infection in a guinea pig model of chorioamnionitis using PAMAM dendrimers[J]. International Journal of Pharmaceutics, 2010, 395 1: Pages 298-308. DOI: 10.1016/j.ijpharm.2010.05.030
[5] MAGDALENA LABIENIEC  Teresa G. Preliminary biological evaluation of poli(amidoamine) (PAMAM) dendrimer G3.5 on selected parameters of rat liver mitochondria[J]. Mitochondrion, 2008, 8 4: Pages 305-312. DOI: 10.1016/j.mito.2008.07.001
[6] TISHA C. KING HEIDEN . Developmental toxicity of low generation PAMAM dendrimers in zebrafish[J]. Toxicology and applied pharmacology, 2007, 225 1: Pages 70-79. DOI: 10.1016/j.taap.2007.07.009
[7] DEBORAH S GOLDBERG P W S Hamidreza Ghandehari. Cellular entry of G3.5 poly (amido amine) dendrimers by clathrin- and dynamin-dependent endocytosis promotes tight junctional opening in intestinal epithelia.[J]. Pharmaceutical Research, 2010, 27 8: 1547-1557. DOI: 10.1007/s11095-010-0153-3