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Purity: ≥98%
Pasireotide acetate (formerly SOM230), the acetate salt of Pasireotide, is a stable cyclohexapeptide somatostatin derivative that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively). It is an orphan drug approved for the treatment of Cushing's disease in patients who fail or are ineligible for surgical therapy. It was developed by Novartis. Pasireotide is a somatostatin analogue with a 40-fold increased affinity to somatostatin receptor 5 compared to other somatostatin analogues.
| ln Vitro |
Pasireotide acetate binds to the human somatostatin receptor (subtype sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9) with a particularly high affinity [1]. GH release in primary cultures of pituitary cells stimulated by growth hormone (GRH) with an IC50 of 0.4 nM [1].
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| ln Vivo |
Pasireotide acetate (160 mg/kg/month; subcutaneously for 4 months) dramatically decreases plasma insulin, boosts plasma plasma levels, reduces tumor growth, and increases Pdx1-Cre cells [2]. Pasireotide acetate (2-50 μg/kg; subcutaneously, twice daily for 42 days) produces analgesic and anti-inflammatory effects via SSTR2 receptors in immune-mediated arthritis models [4].
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| Animal Protocol |
Animal/Disease Models: 12-month-old conditional Men1 gene knockout mice with insulinoma [2]
Doses: 160 mg/kg/oral Route of Administration: monthly subcutaneous injection for 4 months Experimental Results: diminished serum insulin from 1.060 μg/L to 0.3653 μg/L, increasing serum glucose from 4.246 mM to 7.122 mM. Dramatically diminished tumor size and increased apoptosis. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation The excretion of pasireotide into breastmilk has not been studied. However, because it has a high molecular weight of 1047 daltons it is likely to be poorly excreted into breastmilk and it is a peptide that is likely digested in the infant's gastrointestinal tract. It is unlikely to reach the clinically important levels in infant serum. However, the manufacturer states that nursing mothers should not use pasireotide. An alternate drug is preferred. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References |
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| Molecular Formula |
C60H70N10O11
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|---|---|
| Molecular Weight |
1107.26
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| Exact Mass |
1106.522
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| CAS # |
396091-76-2
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| Related CAS # |
Pasireotide L-aspartate salt;396091-77-3;Pasireotide pamoate;396091-79-5;Pasireotide;396091-73-9;Pasireotide (diaspartate);1421446-02-7
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| PubChem CID |
72205932
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
81
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| Complexity |
1970
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| Defined Atom Stereocenter Count |
7
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| SMILES |
CC(=O)O.C1[C@H](CN2[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C2=O)CC3=CC=CC=C3)CC4=CC=C(C=C4)OCC5=CC=CC=C5)CCCCN)CC6=CNC7=CC=CC=C76)C8=CC=CC=C8)OC(=O)NCCN
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| InChi Key |
WFKFNBBHVLMWQH-QKXVGOHISA-N
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| InChi Code |
InChI=1S/C58H66N10O9.C2H4O2/c59-27-13-12-22-46-52(69)64-47(30-38-23-25-42(26-24-38)76-36-39-16-6-2-7-17-39)53(70)66-49(31-37-14-4-1-5-15-37)57(74)68-35-43(77-58(75)61-29-28-60)33-50(68)55(72)67-51(40-18-8-3-9-19-40)56(73)65-48(54(71)63-46)32-41-34-62-45-21-11-10-20-44(41)45;1-2(3)4/h1-11,14-21,23-26,34,43,46-51,62H,12-13,22,27-33,35-36,59-60H2,(H,61,75)(H,63,71)(H,64,69)(H,65,73)(H,66,70)(H,67,72);1H3,(H,3,4)/t43-,46+,47+,48-,49+,50+,51+;/m1./s1
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| Chemical Name |
(3S,6R,9S,12S,15S,19R,20aS)-6-((1H-indol-3-yl)methyl)-9-(4-aminobutyl)-15-benzyl-12-(4-(benzyloxy)benzyl)-1,4,7,10,13,16-hexaoxo-3-phenylicosahydropyrrolo[1,2-a][1,4,7,10,13,16]hexaazacyclooctadecin-19-yl (2-aminoethyl)carbamate acetate
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| Synonyms |
SOM 230; SOM-230; SOM230; trade name: Signifor; Signifor LAR.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~90.31 mM)
H2O : ~1 mg/mL (~0.90 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (2.26 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.26 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2 mg/mL (1.81 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9031 mL | 4.5157 mL | 9.0313 mL | |
| 5 mM | 0.1806 mL | 0.9031 mL | 1.8063 mL | |
| 10 mM | 0.0903 mL | 0.4516 mL | 0.9031 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01329289 | Withdrawn | Drug: SOM230 Drug: Bortezomib Drug: Dexamethasone |
Multiple Myeloma Multiple Myeloma in Relapse |
University of Pittsburgh | 2011-12 | Phase 2 |
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