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396091-73-9,MFCD08067735
Catalog No.:AA00C6E9

396091-73-9 | PASIREOTIDE

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1mg
>98.00%
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$595.00   $417.00
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5mg
>98.00%
3 weeks  
$1,520.00   $1,064.00
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10mg
>98.00%
3 weeks  
$2,293.00   $1,605.00
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  • Technical Information
  • Properties
  • Literature
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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA00C6E9
Chemical Name:
PASIREOTIDE
CAS Number:
396091-73-9
Molecular Formula:
C58H66N10O9
Molecular Weight:
1047.2062
MDL Number:
MFCD08067735
SMILES:
NCCCC[C@@H]1NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H]2N(C(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccc(cc1)OCc1ccccc1)Cc1ccccc1)C[C@@H](C2)OC(=O)NCCN)c1ccccc1)Cc1c[nH]c2c1cccc2
Properties
Computed Properties
 
Complexity:
1940  
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
7  
Heavy Atom Count:
77  
Hydrogen Bond Acceptor Count:
11  
Hydrogen Bond Donor Count:
9  
Rotatable Bond Count:
18  
XLogP3:
4.7  

Literature

Title: Medical treatment of Cushing disease: new targets, new hope.

Journal: Endocrinology and metabolism clinics of North America 20150301

Title: Involvement of bone morphogenetic protein activity in somatostatin actions on ovarian steroidogenesis.

Journal: The Journal of steroid biochemistry and molecular biology 20130301

Title: Multiple once-daily subcutaneous doses of pasireotide were well tolerated in healthy male volunteers: a randomized, double-blind, placebo-controlled, cross-over, Phase I study.

Journal: Endocrine 20121001

Title: Phase I study of pasireotide (SOM 230) and everolimus (RAD001) in advanced neuroendocrine tumors.

Journal: Endocrine-related cancer 20121001

Title: Pasireotide (SOM230) shows efficacy and tolerability in the treatment of patients with advanced neuroendocrine tumors refractory or resistant to octreotide LAR: results from a phase II study.

Journal: Endocrine-related cancer 20121001

Title: Pasireotide (SOM230) protects the retina in animal models of ischemia induced retinopathies.

Journal: Experimental eye research 20121001

Title: Medical management of Cushing's disease: what is the future?

Journal: Pituitary 20120901

Title: Pasireotide.

Journal: Nature reviews. Drug discovery 20120801

Title: Pasireotide (SOM230), a novel multireceptor-targeted somatostatin analogue, is well tolerated when administered as a continuous 7-day subcutaneous infusion in healthy male volunteers.

Journal: Journal of clinical pharmacology 20120701

Title: Safety, tolerability, and pharmacokinetics of a single dose of pasireotide long-acting release in healthy volunteers: a single-center Phase I study.

Journal: European journal of endocrinology 20120501

Title: The hypercoagulable state in Cushing's disease is associated with increased levels of procoagulant factors and impaired fibrinolysis, but is not reversible after short-term biochemical remission induced by medical therapy.

Journal: The Journal of clinical endocrinology and metabolism 20120401

Title: A 12-month phase 3 study of pasireotide in Cushing's disease.

Journal: The New England journal of medicine 20120308

Title: Tolerability and dose proportional pharmacokinetics of pasireotide administered as a single dose or two divided doses in healthy male volunteers: a single-center, open-label, ascending-dose study.

Journal: Clinical therapeutics 20120301

Title: Advances in medical therapies for Cushing's syndrome.

Journal: Discovery medicine 20120201

Title: [Endocrinology].

Journal: Revue medicale suisse 20120111

Title: Effects of somatostatin analogs on glucose homeostasis in rats.

Journal: The Journal of endocrinology 20120101

Title: A first-in-man study to evaluate the safety, tolerability, and pharmacokinetics of pasireotide (SOM230), a multireceptor-targeted somatostatin analog, in healthy volunteers.

Journal: Drug design, development and therapy 20120101

Title: A transplantable phosphorylation probe for direct assessment of G protein-coupled receptor activation.

Journal: PloS one 20120101

Title: SOM230 in Cushing's disease complicated by poorly controlled diabetes mellitus.

Journal: Journal of endocrinological investigation 20111001

Title: Differential antiinflammatory and antinociceptive effects of the somatostatin analogs octreotide and pasireotide in a mouse model of immune-mediated arthritis.

Journal: Arthritis and rheumatism 20110801

Title: SOM230 combined with celecoxib prolongs the survival in nude mice with HepG-2 xenografts.

Journal: Cancer biology & therapy 20110701

Title: Somatostatin receptors in non-neuroendocrine malignancies: the potential role of somatostatin analogs in solid tumors.

Journal: Future oncology (London, England) 20110701

Title: Somatostatin receptor expression in adrenocortical tumors and effect of a new somatostatin analog SOM230 on hormone secretion in vitro and in ex vivo adrenal cells.

Journal: Journal of endocrinological investigation 20110601

Title: Ligand-dependent mechanisms of sst2A receptor trafficking: role of site-specific phosphorylation and receptor activation in the actions of biased somatostatin agonists.

Journal: Molecular endocrinology (Baltimore, Md.) 20110601

Title: [Role of somatostatin receptor ligands in the treatment of acromegaly--literature review].

Journal: Orvosi hetilap 20110501

Title: Transient efficacy of octreotide and pasireotide (SOM230) treatment in GIP-dependent Cushing's syndrome.

Journal: Hormone and metabolic research = Hormon- und Stoffwechselforschung = Hormones et metabolisme 20110401

Title: Pasireotide, an IGF-I action inhibitor, prevents growth hormone and estradiol-induced mammary hyperplasia.

Journal: Pituitary 20110301

Title: Pituitary tumors in 2010: a new therapeutic era for pituitary tumors.

Journal: Nature reviews. Endocrinology 20110201

Title: Prevention of breast cancer: the case for studying inhibition of IGF-1 actions.

Journal: Annals of oncology : official journal of the European Society for Medical Oncology 20110101

Title: Effect of SOM230 (pasireotide) on corticotropic cells: action in dogs with Cushing's disease.

Journal: Neuroendocrinology 20110101

Title: SOM230 (pasireotide) and temozolomide achieve sustained control of tumour progression and ACTH secretion in pituitary carcinoma with widespread metastases.

Journal: Experimental and clinical endocrinology & diabetes : official journal, German Society of Endocrinology [and] German Diabetes Association 20101101

Title: Biological targeted therapies in patients with advanced enteropancreatic neuroendocrine carcinomas.

Journal: Cancer treatment reviews 20101101

Title: Absence of somatostatin SST(2) receptor internalization in vivo after intravenous SOM230 application in the AR42J animal tumor model.

Journal: European journal of pharmacology 20101010

Title: Pharmacological management of acromegaly: a current perspective.

Journal: Neurosurgical focus 20101001

Title: Comment on 'Non-surgical treatment of hormone-secreting pituitary tumors'.

Journal: Journal of clinical neuroscience : official journal of the Neurosurgical Society of Australasia 20100901

Title: Pasireotide (SOM230) demonstrates efficacy and safety in patients with acromegaly: a randomized, multicenter, phase II trial.

Journal: The Journal of clinical endocrinology and metabolism 20100601

Title: Pasireotide alone or with cabergoline and ketoconazole in Cushing's disease.

Journal: The New England journal of medicine 20100513

Title: Effect of everolimus on cell viability in nonfunctioning pituitary adenomas.

Journal: The Journal of clinical endocrinology and metabolism 20100201

Title: Twelve years of the Spanish acromegaly registry: a historical view of acromegaly management in Spain.

Journal: Endocrinologia y nutricion : organo de la Sociedad Espanola de Endocrinologia y Nutricion 20100201

Title: Agonist-biased signaling at the sst2A receptor: the multi-somatostatin analogs KE108 and SOM230 activate and antagonize distinct signaling pathways.

Journal: Molecular endocrinology (Baltimore, Md.) 20100101

Title: ZM447439, a novel promising aurora kinase inhibitor, provokes antiproliferative and proapoptotic effects alone and in combination with bio- and chemotherapeutic agents in gastroenteropancreatic neuroendocrine tumor cell lines.

Journal: Neuroendocrinology 20100101

Title: Novel medical therapies for pituitary tumors.

Journal: Frontiers of hormone research 20100101

Title: Medical treatment of Cushing's disease: somatostatin analogues and pasireotide.

Journal: Neuroendocrinology 20100101

Title: Somatostatin and dopamine receptors.

Journal: Tumori 20100101

Title: [Treatment of pituitary adenomas].

Journal: Orvosi hetilap 20090927

Title: The somatostatin analog SOM230 (pasireotide) ameliorates injury of the intestinal mucosa and increases survival after total-body irradiation by inhibiting exocrine pancreatic secretion.

Journal: Radiation research 20090601

Title: Backbone conformations and side chain flexibility of two somatostatin mimics investigated by molecular dynamics simulations.

Journal: Proteins 20090515

Title: Current therapy and drug pipeline for the treatment of patients with acromegaly.

Journal: Advances in therapy 20090401

Title: [The medical management of Cushing's syndrome].

Journal: Endocrinologia y nutricion : organo de la Sociedad Espanola de Endocrinologia y Nutricion 20090401

Title: Differential effects of octreotide and pasireotide on somatostatin receptor internalization and trafficking in vitro.

Journal: The Journal of clinical endocrinology and metabolism 20090201

Title: Effects of somatostatin analogs on a growth hormone-releasing hormone secreting bronchial carcinoid, in vivo and in vitro studies.

Journal: The Journal of clinical endocrinology and metabolism 20090201

Title: Treatment of pituitary-dependent Cushing's disease with the multireceptor ligand somatostatin analog pasireotide (SOM230): a multicenter, phase II trial.

Journal: The Journal of clinical endocrinology and metabolism 20090101

Title: Impact of Octreotide and SOM-230 on liver metastasis and hepatic lipidperoxidation in ductal pancreatic adenocarcinoma in Syrian Hamster.

Journal: Clinical & experimental metastasis 20090101

Title: Expression of somatostatin receptors in human melanoma cell lines: effect of two different somatostatin analogues, octreotide and SOM230, on cell proliferation.

Journal: The Journal of international medical research 20090101

Title: Modulation of the neuronal response to ischaemia by somatostatin analogues in wild-type and knock-out mouse retinas.

Journal: Journal of neurochemistry 20080901

Title: Effects of somatostatin analog SOM230 on cell proliferation, apoptosis, and catecholamine levels in cultured pheochromocytoma cells.

Journal: Journal of molecular endocrinology 20080601

Title: Pasireotide (SOM230): development, mechanism of action and potential applications.

Journal: Molecular and cellular endocrinology 20080514

Title: Somatostatinergic ligands in dopamine-sensitive and -resistant prolactinomas.

Journal: European journal of endocrinology 20080501

Title: Pituitary-targeted medical therapy of Cushing's disease.

Journal: Expert opinion on investigational drugs 20080501

Title: [Management of patients with neuroendocrine tumors of the esophagus, stomach, and duodenum].

Journal: Nihon Geka Gakkai zasshi 20080501

Title: Preclinical evidences suggest new treatment options for endocrine disorders: Pasireotide (SOM230) and Everolimus (RAD001).

Journal: Annales d'endocrinologie 20080401

Title: Modulation of expression of somatostatin receptor subtypes in Graves' ophthalmopathy orbits: relevance to novel analogs.

Journal: American journal of physiology. Endocrinology and metabolism 20071201

Title: Pasireotide--a somatostatin analog for the potential treatment of acromegaly, neuroendocrine tumors and Cushing's disease.

Journal: IDrugs : the investigational drugs journal 20071201

Title: Octreotide and the novel multireceptor ligand somatostatin receptor agonist pasireotide (SOM230) block the adrenalectomy-induced increase in mitotic activity in male rat anterior pituitary.

Journal: Endocrinology 20070601

Title: SOM230, a new somatostatin analogue, is highly effective in the therapy of growth hormone/prolactin-secreting pituitary adenomas.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20070501

Title: Regulation of insulin and glucagon secretion from rat pancreatic islets in vitro by somatostatin analogues.

Journal: Regulatory peptides 20070110

Title: Inhibitory effect of pasireotide and octreotide on lymphocyte activation.

Journal: Journal of neuroimmunology 20070101

Title: Somatostatin receptor subtypes in human non-functioning neuroendocrine tumors and effects of somatostatin analogue SOM230 on cell proliferation in cell line NCI-H727.

Journal: Anticancer research 20070101

Title: Somatostatin analogues stimulate p27 expression and inhibit the MAP kinase pathway in pituitary tumours.

Journal: European journal of endocrinology 20060801

Title: SOM230 inhibits insulin-like growth factor-I action in mammary gland development by pituitary independent mechanism: mediated through somatostatin subtype receptor 3?

Journal: Molecular endocrinology (Baltimore, Md.) 20060201

Title: New aspects in the diagnosis and treatment of Cushing disease.

Journal: Frontiers of hormone research 20060101

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20051201

Title: Regulation of CRH-induced secretion of ACTH and corticosterone by SOM230 in rats.

Journal: European journal of endocrinology 20050901

Title: Distinct functional properties of native somatostatin receptor subtype 5 compared with subtype 2 in the regulation of ACTH release by corticotroph tumor cells.

Journal: American journal of physiology. Endocrinology and metabolism 20050801

Title: The somatostatin analogue SOM230, compared with octreotide, induces differential effects in several metabolic pathways in acromegalic patients.

Journal: Clinical endocrinology 20050801

Title: Pharmacokinetic-pharmacodynamic comparison of a novel multiligand somatostatin analog, SOM230, with octreotide in patients with acromegaly.

Journal: Clinical pharmacology and therapeutics 20050701

Title: Regulation of ghrelin secretion by somatostatin analogs in rats.

Journal: European journal of endocrinology 20050601

Title: Somatostatin receptors 2 and 5 are preferentially expressed in proliferating endothelium.

Journal: British journal of cancer 20050425

Title: The multi-ligand somatostatin analogue SOM230 inhibits ACTH secretion by cultured human corticotroph adenomas via somatostatin receptor type 5.

Journal: European journal of endocrinology 20050401

Title: Pharmacologic therapies for acromegaly: a review of their effects on glucose metabolism and insulin resistance.

Journal: Treatments in endocrinology 20050101

Title: Primary therapy for acromegaly with somatostatin analogs and a discussion of novel peptide analogs.

Journal: Reviews in endocrine & metabolic disorders 20050101

Title: Medicinal chemistry of somatostatin analogs leading to the DTPA and DOTA conjugates of the multi-receptor-ligand SOM230.

Journal: Journal of endocrinological investigation 20050101

Title: Short- and long-term effects of octreotide and SOM230 on GH, IGF-I, ACTH, corticosterone and ghrelin in rats.

Journal: Journal of endocrinological investigation 20050101

Title: Efficacy and limits of somatostatin analogs.

Journal: Journal of endocrinological investigation 20050101

Title: New perspectives in the medical treatment of acromegaly.

Journal: Journal of endocrinological investigation 20050101

Title: Novel molecular aspects of pituitary adenomas.

Journal: Journal of endocrinological investigation 20050101

Title: Potential indications for somatostatin analogs in Cushing's syndrome.

Journal: Journal of endocrinological investigation 20050101

Title: Inhibition of endothelial proliferation by the somatostatin analogue SOM230.

Journal: Clinical endocrinology 20041001

Title: The novel somatostatin ligand (SOM230) regulates human and rat anterior pituitary hormone secretion.

Journal: The Journal of clinical endocrinology and metabolism 20040601

Title: The novel somatostatin analog SOM230 is a potent inhibitor of hormone release by growth hormone- and prolactin-secreting pituitary adenomas in vitro.

Journal: The Journal of clinical endocrinology and metabolism 20040401

Title: A single-dose comparison of the acute effects between the new somatostatin analog SOM230 and octreotide in acromegalic patients.

Journal: The Journal of clinical endocrinology and metabolism 20040201

Title: Functional activity of the multiligand analog SOM230 at human recombinant somatostatin receptor subtypes supports its usefulness in neuroendocrine tumors.

Journal: Neuroendocrinology 20040101

Title: The role of somatostatin analogs in Cushing's disease.

Journal: Pituitary 20040101

Title: New insights on SOM230, a universal somatostatin receptor ligand.

Journal: Journal of endocrinological investigation 20030101

Title: SOM230: a new somatostatin peptidomimetic with potent inhibitory effects on the growth hormone/insulin-like growth factor-I axis in rats, primates, and dogs.

Journal: Endocrinology 20021001

Title: New somatostatin analogs: will they fulfil old promises?

Journal: European journal of endocrinology 20020501

Title: SOM230: a novel somatostatin peptidomimetic with broad somatotropin release inhibiting factor (SRIF) receptor binding and a unique antisecretory profile.

Journal: European journal of endocrinology 20020501

Title: Pasireotide and octreotide stimulate distinct patterns of sst2A somatostatin receptor phosphorylation.

Journal: Molecular endocrinology (Baltimore, Md.)

Title: Structural determinants of agonist-selective signaling at the sst(2A) somatostatin receptor.

Journal: Molecular endocrinology (Baltimore, Md.)

Title: 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.

Title: 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.

Title: Schmid HA, et, al. Pasireotide (SOM230): development, mechanism of action and potential applications. Mol Cell Endocrinol. 2008 May 14;286(1-2):69-74.

Title: 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.

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