Cyclosporine

Catalog No.S1514

Cyclosporine  Chemical Structure

Molecular Weight(MW): 1202.61

Cyclosporine is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation.

Size Price Stock Quantity  
In DMSO USD 480 In stock
USD 120 In stock
USD 370 In stock
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Biological Activity

Description Cyclosporine is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation.
Targets
calcineurin phosphatase [2]
In vitro

Cyclosporine induces phenotypic changes, including invasiveness of non-transformed cells, by a cell-autonomous mechanism. Cyclosporine treatment of adenocarcinoma cells results in striking morphological alterations, including membrane ruffling and numerous pseudopodial protrusions, increased cell motility, and anchorage-independent (invasive) growth. [1] Cyclosporine (cyclosporin A, CsA) has potent immunosuppressive properties, reflecting its ability to block the transcription of cytokine genes in activated T cells. Cyclosporine through formation of a complex with cyclophilin inhibits the phosphatase activity of calcineurin, which regulates nuclear translocation and subsequent activation of NFAT transcription factors. Cyclosporine also blocks the activation of JNK and p38 signaling pathways triggered by antigen recognition, making CsA a highly specific inhibitor of T cell activation. [2] Cyclosporine-mediated inhibition of the biliary excretion of MPAG by the Mrp2 transporter is the mechanism responsible for the interaction between Cyclosporine and mycophenolate mofetil (MMF). [3] Cyclosporine inhibits biochemical and morphological differentiation of skeletal muscle cells while having a minimal effect on proliferation. [4]

In vivo Cyclosporine enhances tumour growth in immunodeficient SCID-beige mice. [1] Cyclosporine inhibits muscle regeneration after induced trauma in mice. [4] Cyclosporine peaks at 1 hour in blood, spleen, and kidney, with higher concentrations in spleen and kidney than in blood. [5]

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (83.15 mM)
Ethanol 100 mg/mL (83.15 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 1202.61
Formula

C62H111N11O12

CAS No. 79217-60-0
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01503242 Recruiting Plasma Cell Myeloma|Refractory Plasma Cell Myeloma Fred Hutchinson Cancer Research Center|National Cancer Institute (NCI) January 9, 2012 Phase 1
NCT01623167 Recruiting Aplastic Anemia|Neutropenia|Pancytopenia|Anemia|Thrombocytopenia National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) June 7, 2012 Phase 1|Phase 2
NCT00977977 Recruiting Nephrotic Syndrome|Proteinuria|Autoimmune Disease|Glomerular Disease|Membranous Glomerulonephritis National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC) August 28, 2009 Phase 2
NCT00425802 Completed Leukemia|Lymphoma Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) November 28, 2006 Phase 2
NCT00260689 Completed Immunosuppresion|Thrombocytopenia|Pancytopenia|Neutropenia National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) November 28, 2005 Phase 2
NCT00723099 Suspended Acute Biphenotypic Leukemia|Acute Lymphoblastic Leukemia|Acute Myeloid Leukemia|Aggressive Non-Hodgkin Lymphoma|Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Chronic Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Indolent Non-Hodgkin Lymphoma|Malignant Lymphoma, Large Cell Type|Mixed Phenotype Acute Leukemia|Myelodysplastic Syndrome|Myeloproliferative Neoplasm|Recurrent Chronic Lymphocytic Leukemia|Recurrent Follicular Lymphoma|Recurrent Lymphoplasmacytic Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Plasma Cell Myeloma|Recurrent Small Lymphocytic Lymphoma|Recurrent T-Cell Non-Hodgkin Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Refractory Follicular Lymphoma|Refractory Hodgkin Lymphoma|Refractory Lymphoplasmacytic Lymphoma|Refractory Mantle Cell Lymphoma|Refractory Small Lymphocytic Lymphoma|T-Cell Non-Hodgkin Lymphoma Fred Hutchinson Cancer Research Center|National Cancer Institute (NCI) June 25, 2008 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    What is the difference between S2286 (cyclosporin A) and S1514 (cyclosporin)?

  • Answer:

    Cyclosporine is a mixture of Cyclosporine A, derivatives of Cyclosporine A, salts of Cyclosporine A. Cyclosporine A is an especially useful Cyclosporine component.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID