[CAS NO. ] Pasireotideditrifluoroacetate

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PRODUCTS SPECIFICATIONS

Catalog

HY-79135

Brand

MCE

CAS

DESCRIPTION

Overview

MDL	-
Molecular Weight	1275.25
Molecular Formula	C62H68F6N10O13
SMILES	O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.NCCCC[C@@H](C(N[C@H]1CC2=CC=C(C=C2)OCC3=CC=CC=C3)=O)NC([C@H](NC([C@H](C4=CC=CC=C4)NC([C@H]5N(C([C@H](CC6=CC=CC=C6)NC1=O)=O)C[C@H](OC(NCCN)=O)C5)=O)=O)CC7=CNC8=C7C=CC=C8)=O

For research use only. We do not sell to patients.

5 Publications Citing Use of MCE

Summary

Pasireotide (SOM230) ditrifluoroacetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5 , pK _i =8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide ditrifluoroacetate exhibits antisecretory, antiproliferative, and proapoptotic activity ^[1] ^[2] .

IC50 & Target

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

In Vitro

Pasireotide ditrifluoroacetate exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pK _i =8.2/9.0/9.1/<7.0/9.9, respectively) ^[1] .
Pasireotide ditrifluoroacetate effectively inhibits the growth hormone releasing hormone (GHRH) induced growth hormone (GH) release in primary cultures of rat pituitary cells, with an IC ₅₀ of 0.4 nM ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Pasireotide ditrifluoroacetate (160 mg/kg/mouth; s.c. for 4 months) significantly decreases the serum insulin, increases serum glucose, reduces the tumor size and increases apoptosis in Pdx1-Cre ^[2] .
Pasireotide ditrifluoroacetate (2-50 μg/kg; s.c. twice daily for 42 days) exerts the antinociceptive and antiinflammatory actions via the SSTR2 receptor in a mouse model of immune-mediated arthritis ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	12 month-old conditional Men1 knockout mice with insulinoma ^[2]
Dosage:	160 mg/kg/mouth
Administration:	S.c. every month for 4 months
Result:	Decreased the serum insulin from 1.060 μg/L to 0.3653 μg/L and increased the serum glucose from 4.246 mM to 7.122 mM. Significantly reduced the tumor size and increased apoptosis.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00088608	Novartis Pharmaceuticals\|Novartis	Cushing´s Syndrome	April 2004	Phase 2
NCT01670110	Mayo Clinic	Somatostatin Analogs\|Polycystic Liver Disease\|Autosomal Dominant Polycystic Kidney Disease\|Autosomal Dominant Polycystic Liver Disease	August 2012	Phase 2
NCT01234974	Milton S. Hershey Medical Center	Multiple Myeloma	December 2010	Phase 2
NCT00434148	Novartis Pharmaceuticals\|Novartis	Cushing´s Disease	December 2006	Phase 3
NCT03080181	University of Palermo	Cushing Disease	May 2013	Phase 4
NCT02835131	Montefiore Medical Center	Congenital Hyperinsulinism
NCT02775227	Helsinki University Central Hospital	Pancreatic Fistula\|Pancreatic Neoplasms	May 2016	Phase 4
NCT00958841	Novartis Pharmaceuticals\|Novartis	Pancreatic Neoplasm\|Pituitary Neoplasm\|Nelson Syndrome\|Ectopic ACTH Syndrome	September 2009	Phase 2
NCT01356862	Alliance Pour La Recherche en Cancerologie	Breast Cancer	September 2010	Phase 2
NCT02668172	Erasmus Medical Center\|Novartis	Acromegaly	August 2015	Phase 4
NCT04281680	Helsinki University Central Hospital	Surgical Complications	July 1, 2014
NCT01625520	Federico II University	Medullary Thyroid Cancer	February 2012	Phase 2
NCT01639352	Lynn Feun\|University of Miami	Hepatocellular Carcinoma	July 2012	Phase 2
NCT02021942	Prof. Dr. Berthold Schalke\|Crolll Gmbh\|University of Regensburg	Primary Inoperable Thymoma\|Local Recurrent Thymoma	March 2012	Phase 2
NCT01995734	Novartis Pharmaceuticals\|Novartis	Acromegaly
NCT01252251	Memorial Sloan Kettering Cancer Center\|Novartis Pharmaceuticals	Uveal Melanoma	November 2010	Phase 2
NCT00171730	Novartis Pharmaceuticals\|Novartis	Acromegaly	August 24, 2004	Phase 2
NCT02779257	University of Maryland, Baltimore\|Novartis	Gastro-enteropancreatic Neuroendocrine Tumor	April 2016	Phase 4
NCT02780882	Cedars-Sinai Medical Center\|Novartis	Ectopic ACTH Syndrome	December 2015	Phase 2
NCT01578928	Novartis Pharmaceuticals\|Novartis	Renal Impairment	May 2012	Phase 1
NCT02310269	RECORDATI GROUP	Cushings Disease	March 28, 2013
NCT02619617	Novartis Pharmaceuticals\|Novartis	Cluster Headache - Episodic and Chronic	October 31, 2016	Phase 2
NCT01488487	UNC Lineberger Comprehensive Cancer Center\|Novartis Pharmaceuticals	Advanced Adult Hepatocellular Carcinoma	December 2011	Phase 2
NCT01617733	Sheffield Teaching Hospitals NHS Foundation Trust\|Novartis\|The Christie NHS Foundation Trust\|Oxford University Hospitals NHS Trust\|Barts & The London NHS Trust	Nelson Syndrome	March 2011	Phase 2
NCT03103009	University of Colorado, Denver\|Novartis	Hyperinsulinemic Hypoglycemia\|Post Gastrointestinal Tract Surgery Hypoglycaemia	March 22, 2017	Phase 1
NCT01270321	Emory University\|Novartis	Thyroid Cancer	November 2010	Phase 2
NCT01263353	Novartis Pharmaceuticals\|Novartis	Gastroenteropancreatic Neuroendocrine Tumor of the Pulmonary ot Gastroenteropancreatic System	November 2010	Phase 1
NCT01374451	Novartis Pharmaceuticals\|Novartis	Islet Cell Tumor	June 2011	Phase 2
NCT01652547	Novartis Pharmaceuticals\|Novartis	Metastatic Melanoma and Merkel Cell Carcinoma	November 2012	Phase 1
NCT02713776	Hospices Civils de Lyon	Enterostomy	December 13, 2016	Phase 2
NCT01313559	Sidney Kimmel Cancer Center at Thomas Jefferson University\|Novartis Pharmaceuticals\|Thomas Jefferson University	Castrate Resistant Prostate Cancer\|Chemotherapy Naive Prostate Cancer\|Prostate Cancer	June 2011	Phase 2
NCT01582061	Novartis Pharmaceuticals\|Novartis	Cushing´s Disease	August 16, 2011	Phase 3
NCT01468532	Barbara Ann Karmanos Cancer Institute\|National Cancer Institute (NCI)	Adenocarcinoma of the Prostate\|Hormone-resistant Prostate Cancer\|Recurrent Prostate Cancer\|Stage IV Prostate Cancer	October 2011	Phase 1\|Phase 2
NCT01895296	Universitaire Ziekenhuizen KU Leuven	Postoperative Dumping Syndrome	September 2008	Phase 2
NCT01794793	RECORDATI GROUP	Cushing´s Disease\|Acromegaly\|Neuroendocrine Tumors\|Pituitary Tumors\|Ectopic ACTH Secreting (EAS) Tumors\|Dumping Syndrome\|Prostate Cancer\|Melanoma Negative for bRAF\|Melanoma Negative for nRAS	June 10, 2013	Phase 4
NCT00804336	Dana-Farber Cancer Institute\|Beth Israel Deaconess Medical Center\|Brigham and Women´s Hospital\|Massachusetts General Hospital\|Novartis	Neuroendocrine Tumor\|Carcinoid Tumor\|Pancreatic Neuroendocrine Tumor	October 2008	Phase 1
NCT01374906	Novartis Pharmaceuticals\|Novartis	Cushing´s Disease	November 4, 2011	Phase 3
NCT01417806	South Florida Veterans Affairs Foundation for Research and Education\|Novartis Pharmaceuticals	Small Cell Lung Cancer	July 2011	Phase 2
NCT02354508	Novartis Pharmaceuticals\|Novartis	Acromegaly	March 31, 2015	Phase 3
NCT00929669	University of Pennsylvania	Gonadotroph Adenomas	June 2009	Phase 2
NCT01637272	Novartis Pharmaceuticals\|Novartis	Dumping Syndrome	January 8, 2013	Phase 2
NCT01469572	Emory University\|Novartis	Neuroendocrine Tumors	December 2011	Phase 1
NCT00171951	Novartis Pharmaceuticals\|Novartis	Cushing Disease	August 13, 2004	Phase 2
NCT00690430	Novartis Pharmaceuticals\|Novartis	Symptomatic Refractory Resistant Carcinoid Disease	April 2008	Phase 3
NCT01329289	University of Pittsburgh\|Novartis	Multiple Myeloma in Relapse\|Multiple Myeloma	December 2011	Phase 2
NCT02048319	Radboud University Medical Center	Symptomatic Dominant Liver Cyst	December 2013	Phase 3
NCT01563354	Novartis Pharmaceuticals\|Novartis	Neuroendocrine Carcinoma of the Lung and Thymus	August 16, 2013	Phase 2
NCT01137682	Novartis Pharmaceuticals\|Novartis	Acromegaly	July 19, 2010	Phase 3
NCT00088582	Novartis Pharmaceuticals\|Novartis	Acromegaly	March 2004	Phase 2
NCT03847207	Heptares Therapeutics Limited	Healthy	February 13, 2019	Phase 1
NCT02622906	Robert Benamouzig\|Hospital Avicenne	Angiodysplasia	March 2012	Phase 2
NCT02749227	Columbia University	Pituitary Tumor\|ACTH-producing Pituitary Tumour	July 10, 2017	Phase 2
NCT01620138	Universidade Federal do Rio de Janeiro	Non-functioning Pituitary Adenomas\|Prolactinomas	March 2010	Phase 2\|Phase 3
NCT02215070	Anthony Sung, MD\|Massachusetts General Hospital\|Duke University	Hematological Malignancies	January 21, 2015	Phase 2
NCT02060383	Novartis Pharmaceuticals\|Novartis	Cushing´s Disease\|Acromegaly	May 23, 2014	Phase 4
NCT01646684	Novartis Pharmaceuticals\|Novartis	Castration Resistant Prostate Cancer	March 8, 2013	Phase 1
NCT01128192	Robert R. Henry, MD\|Veterans Medical Research Foundation	Hyperglycemia	August 2009	Phase 2
NCT00446082	Novartis Pharmaceuticals\|Novartis	Carcinoid Tumor\|Acromegaly	June 2006	Phase 1
NCT03514576	Zealand University Hospital	Hypoglycemia, Reactive	June 1, 2018	Phase 4
NCT01253161	H. Lee Moffitt Cancer Center and Research Institute\|Novartis Pharmaceuticals\|RECORDATI GROUP	Neuroendocrine Tumors\|Carcinoid Tumors	February 1, 2011	Phase 2
NCT00088595	Novartis Pharmaceuticals\|Novartis	Carcinoid Tumors	January 2004	Phase 2
NCT03053284	Montefiore Medical Center\|Novartis Pharmaceuticals	Congenital Hyperinsulinism\|Insulinoma\|Hyperinsulinism	April 2017	Phase 2
NCT04826432	Gustave Roussy, Cancer Campus, Grand Paris	Peritoneal Carcinomatosis	September 3, 2020	Phase 2
NCT01915303	Novartis Pharmaceuticals\|Novartis	Cushings Disease	March 6, 2014	Phase 2
NCT01372618	NYU Langone Health	Ductal Carcinoma in Situ	June 2011	Phase 1\|Phase 2
NCT00600886	Novartis Pharmaceuticals\|Novartis	Acromegaly	February 11, 2008	Phase 3
NCT01364415	Novartis Pharmaceuticals\|Novartis	Neuroendocrine Tumors	August 2011	Phase 1
NCT00994110	Memorial Sloan Kettering Cancer Center\|Novartis Pharmaceuticals	Pancreatic Cancer	October 2009	Phase 3
NCT01673646	Novartis Pharmaceuticals\|Novartis	Acromegaly\|Pituitary Gigantism	October 16, 2012	Phase 2
NCT01590199	Novartis Pharmaceuticals\|Novartis	Neuroendocrine Tumors	May 18, 2012	Phase 1
NCT02527993	Zealand University Hospital	Hypoglycemia\|Obesity\|Surgery	October 2015	Phase 4
NCT01385956	H. Lee Moffitt Cancer Center and Research Institute\|Novartis Pharmaceuticals	Pancreatic Cancer	June 2011	Phase 1
NCT01283542	Novartis Pharmaceuticals\|Novartis	Non-functioning Pituitary Adenoma	November 26, 2012	Phase 2
NCT01372644	NYU Langone Health\|United States Department of Defense	Atypical Ductal Breast Hyperplasia\|Lobular Carcinoma in Situ (LCIS)\|Atypical Lobular Hyperplasia (ALH) of Breast	November 2007	Phase 1
NCT00698464	Novartis Pharmaceuticals\|Novartis	Hepatic Cirrhosis\|Alcoholism	July 2008	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 78.42 mM ; Need ultrasonic)

H ₂ O : 33.33 mg/mL ( 26.14 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.7842 mL	3.9208 mL	7.8416 mL
5 mM	0.1568 mL	0.7842 mL	1.5683 mL
10 mM	0.0784 mL	0.3921 mL	0.7842 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (1.96 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (1.96 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (1.96 mM); Clear solution

* All of the co-solvents are available by MCE.