Ascomycin (FK520)

Catalog No.S7411 Batch:S741103

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Technical Data

Formula

C43H69NO12
Molecular Weight 792.01 CAS No. 104987-12-4
Solubility (25°C)* In vitro DMSO 100 mg/mL (126.26 mM)
Ethanol 100 mg/mL (126.26 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
1.65mg/ml Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Ascomycin (FK520, FR 900520, Immunomycin), an FK-506 analog, is a neutral macrolide immunosuppressant, which prevents rejection after an organ transplant. Phase 3.
Targets
calcineurin phosphatase [2]
49 nM
In vitro Ascomycin, isolated from Streptomyces, suppresses immune response in vitro with IC50 of 0.55 nM for mouse mixed lymphocyte. [1] Ascomycin inhibits calcineurin phosphatase with IC50 of 49 nM through formation of an FKBP12-FK520-calcineurin ternary complex. FK520 also accelerate the rate of nerve regeneration, and promotes neurite outgrowth. [2] Ascomycin shows antimalarial effects via inhibition of the chaperone activity of this bifunctional protein. [3]
In vivo Ascomycin (3.2 mg/kg, i.m.) clearly prolongs skin allograft survival in rats. [1] Ascomycin, at 50 or 100 μM, produces anticonvulsant effect against picrotoxin-induced seizures when infused into the rat hippocampus. [4]

Protocol (from reference)

Animal Study:[1]
  • Animal Models

    Recipient WKA rats transplanted with F344 skin allografts.

  • Dosages

    ~32 mg/kg 5 days a week.

  • Administration

    i.m.

Selleck's Ascomycin (FK520) has been cited by 2 publications

Tacrolimus and ascomycin inhibit melanoma cell growth, migration and invasion via targeting nuclear factor of activated T-cell 3 [ Melanoma Res, 2020, 30(4):325-335] PubMed: 32301802
The Establishment and Validation of the Human U937 Cell Line as a Cellular Model to Screen Immunomodulatory Agents Regulating Cytokine Release Induced by Influenza Virus Infection [ Virol Sin, 2019, 34(6):648-661] PubMed: 31286365

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.