202009-66-3

PAMAM dendrimer G4.5 carboxylate (PAMAM G4.5 carboxylate) is a polyamidoamine (PAMAM) dendrimer with carboxylate termini that has been used as a drug delivery system.1 It is approximately 87.9 Å in diameter in water and has 96 surface groups.2 Unlike the amine-terminated PAMAM G5.0 (Item No. 39075), it does not rupture bilayer lipid membranes when used at a concentration of 50 µM.3 PAMAM G4.5 carboxylate disulfur-linked aggregates (10 µg/ml) encapsulating the phenol ferulic acid (Item No. 19871) and the mitotic inhibitor paclitaxel (Item No. 10461) induce apoptosis and decrease the mitochondrial membrane potential in multidrug-resistant KB-8-5 epidermal carcinoma cells.1 Complexes of PAMAM G4.5 carboxylate with the active component of cisplatin are cytotoxic to A2780 ovarian cancer cells (IC50 = 620 nM).4 A fluorescently labeled form of PAMAM G4.5 carboxylate selectively accumulates in tumors and kidneys over liver, spleen, heart, and lungs in a 4T1 murine mammary carcinoma model.5WARNING This product is not for human or veterinary use.

[1] RAJESHKUMAR ANBAZHAGAN. PAMAM G4.5 dendrimers for targeted delivery of ferulic acid and paclitaxel to overcome P-glycoprotein-mediated multidrug resistance[J]. Biotechnology and Bioengineering, 2020, 118 3: 1213-1223. DOI: 10.1002/bit.27645
[2] 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
[3] DZMITRY SHCHARBIN. The breakdown of bilayer lipid membranes by dendrimers.[J]. Cellular & Molecular Biology Letters, 2006, 11 2: 242-248. DOI: 10.2478/s11658-006-0018-2
[4] GORDON J. KIRKPATRICK . Evaluation of anionic half generation 3.5–6.5 poly(amidoamine) dendrimers as delivery vehicles for the active component of the anticancer drug cisplatin[J]. Journal of Inorganic Biochemistry, 2011, 105 9: Pages 1115-1122. DOI: 10.1016/j.jinorgbio.2011.05.017
[5] NATALIA ODDONE. In vitro and in vivo uptake studies of PAMAM G4.5 dendrimers in breast cancer.[J]. Journal of Nanobiotechnology, 2016, 14 1: 45. DOI: 10.1186/s12951-016-0197-6