<Suppliers Price>

Pasireotide Pamoate

Names

[ CAS No. ]:
396091-79-5

[ Name ]:
Pasireotide Pamoate

[Synonym ]:
4,4'-Methylenebis(3-hydroxy-2-naphthoic acid) - cyclo[(2S)-2-phenylglycyl-D-tryptophyl-L-lysyl-O-benzyl-L-tyrosyl-L-phenylalanyl-(4R)-4-{[(2-aminoethyl)carbamoyl]oxy}-L-prolyl] (1:1)
2-Naphthalenecarboxylic acid, 4,4'-methylenebis[3-hydroxy-, compd. with cyclo[(2S)-2-phenylglycyl-D-tryptophyl-L-lysyl-O-(phenylmethyl)-L-tyrosyl-L-phenylalanyl-(4R)-4-[[[(2-aminoethyl)amino]carbonyl]oxy]-L-prolyl] (1:1)

Biological Activity

[Description]:

Pasireotide pamoate (SOM230 pamoate) is a stable cyclohexapeptide somatostatin mimic that improves agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively). Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity[1][2].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> GPCR/G Protein >> Somatostatin Receptor

[Target]

pKi: 8.2 (sst1), 9.0 (sst2), 9.1 (sst3), <7.0 (sst4), 9.9 (sst5)[1]


[In Vitro]

Pasireotide pamoate exhibits unique high-affinity binding to human somatostatin receptors[1]. Pasireotide pamoate effectively inhibits the growth hormone releasing hormone (GHRH) induced growth hormone (GH) release in primary cultures of rat pituitary cells with an IC50 of 0.4±0.1 nM[1].

[In Vivo]

Pasireotide pamoate (160mg/Kg/month; s.c.; for 4 months) decreases serum insulin levels and increases serum glucose levels in Pdx1-Cre[2]. Pasireotide pamoate displays a reduction in tumor activity and reduces Pancreatic Neuroendocrine Tumor (PNET) size in Pdx1-Cre[2]. Pasireotide pamoate increases apoptosis in PNETs in Pdx1-Cre[2]. Pasireotide pamoate exerts the antinociceptive and antiinflammatory actions via the SSTR2 receptor in in a mouse model of immune-mediated arthritis[3]. Animal Model: Eight 12-month old mice carrying the Men1 allele, Men1 floxed/floxed conditional knockout (Pdx1-Cre)[2] Dosage: 60mg/kg Administration: Subcutaneous injection; very month; for 4 months Result: Decreased serum insulin levels and increases serum glucose levels in Pdx1-Cre.

[References]

[1]. Lewis I, et al. A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential. J Med Chem. 2003 Jun 5;46(12):2334-44.

[2]. Quinn TJ, et al. Pasireotide (SOM230) is effective for the treatment of pancreatic neuroendocrine tumors (PNETs) in a multiple endocrine neoplasia type 1 (MEN1) conditional knockout mouse model. Surgery. 2012 Dec;152(6):1068-77.

[3]. Imhof AK, et al. Differential antiinflammatory and antinociceptive effects of the somatostatin analogs octreotide and pasireotide in a mouse model of immune-mediated arthritis. Arthritis Rheum. 2011 Aug;63(8):2352-62.

Chemical & Physical Properties

[ Molecular Formula ]:
C81H82N10O15

[ Molecular Weight ]:
1435.576

[ Exact Mass ]:
1434.596069

Related Compounds