Zotarolimus(ABT-578)

Catalog No.S7091

Zotarolimus(ABT-578) Chemical Structure

Molecular Weight(MW): 966.21

Zotarolimus (ABT-578) is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM.

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Biological Activity

Description Zotarolimus (ABT-578) is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM.
Features Zotarolimus has a shorter in vivo half-life and is also demonstrated in rats to have less potent systemic immunosuppression than rapamycin.
Targets
FKBP-12 [1]
2.8 nM
In vitro

Zotarolimus (ABT-578) is a semi-synthetic analogue of rapamycin, made by substituting a tetrazole ring for the native hydroxyl group at position 42 in rapamycin. Zotarolimus is highly effective in inhibiting both smooth muscle cell and endothelial cell proliferation, with IC50 values of 2.9 nM and 2.6 nM, respectively. [1] Zotarolimus is mechanistically similar to sirolimus in having high-affinity binding to the immunophilin FKBP12 and comparable potency for inhibiting in vitro proliferation of both human and rat T cells. Zotarolimus inhibits Con A-induced human T cells and rat T cells proliferation with IC50 of 7.0 nM and 1337 nM respectively. [2]

In vivo Zotarolimus-eluting stents effectively reduce neointima formation in a 28-day, well-characterized swine model of coronary artery restenosis. Zotarolimus appears effective in preventing neointimal thickening, reducing late loss from 1.03 to 0.62 mm with a 47% reduction in TVF compared with bare metal stents (15.4% with the Driver stent to 8.1% with the Endeavor stent). [1] Zotarolimus is efficacious in suppressing adjuvant DTH, EAE, and cardiac allograft rejection with ED50 values of 1.72, 1.17, and 3.71 mg/kg/day, respectively. [2]

Protocol

Kinase Assay:

[1]

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Binding Affinity to FKBP12:

96-well microtiter plates are first coated with FKBP-12 CMP-KDO synthetase fusion protein at 10 μg/mL, 100 μL/well for 2-3 h, followed by addition of 50 μL/well of buffer A (2% BSA and 0.2% Tween-20 in D-PBS) for 30-60 min. Microtiter plates are then washed three times with buffer B (0.2% Tween in D-PBS, pH adjusted to 7.4). Fifty microlitres of buffer A (for maximum), 20 μM FK506 in buffer A (for background), or various concentrations of zotarolimus (10 pM-1 μM) in buffer A are added to each well followed by addition of 50 μL of A-79397 (an FK506 analogue)-alkaline phosphatase conjugate in buffer A. Microtiter plates are incubated at room temperature for 2-2.5 h followed by three washes with buffer B. About 100 μL of pNPP (p-nitrophenyl-phosphate) in 0.1 M aminomethylpropanol are added to each well and plates are incubated at room temperature for 90-120 min. Absorbance at 405 nM is read using an ELISA plate
Cell Research:

[1]

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  • Cell lines: Human coronary artery cells
  • Concentrations: ~1 μM
  • Incubation Time: 5 days
  • Method:

    Cell proliferation is assayed by measuring tritiated thymidine incorporation in vitro. Human coronary artery cells (hCa) are seeded into tissue culture flasks for expansion and applied to 96-well plates at desired density in complete media (5000 hCaSMC; 10 000 hCaEC). After 2 days, complete media is replaced with incomplete media to synchronize cells and induce G0 state. Two days later, incomplete media are removed and replaced with complete media (serum/growth factors) to induce G0 to G1 transition. Complete media also contain drug at desired concentrations to determine its effects on cell proliferation. On day 7, 3H-thymidine is added to cells to monitor DNA synthesis, and cells are harvested after overnight incorporation of radioactivity. After an incubation period of 72 h, 25 μL (1 μCi/well) of 3H-thymidine are added to each well. The cells are incubated at 37°C for 16-18 h to allow for incorporation of 3H-thymidine into newly synthesized DNA and the cells harvested onto 96-well plates containing bonded glass fibre filters . The filter plates are air-dried overnight, MicroScint-20 (25 μL) added to each filter well and counted. Drug activity is determined by the inhibition of 3H-thymidine incorporation into newly synthesized DNA relative to cells grown in complete media.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: Male Sprague-Dawley rats
  • Formulation: ethanol: propylene glycol: cremophor EL: D5W vehicle (20: 30: 2: 48, by volume)
  • Dosages: 2.5 mg/kg
  • Administration: intravenous or oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (103.49 mM)
Ethanol 100 mg/mL (103.49 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 966.21
Formula

C52H79N5O12

CAS No. 221877-54-9
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02939976 Not yet recruiting Myocardial Infarction David Kong, M.D.|Medtronic Vascular|Volcano Corporation|Terumo Medical Corporation|Duke University December 2016 --
NCT02770651 Recruiting Coronary Artery Disease|Coronary Disease|Myocardial Ischemia|Arterial Occlusive Diseases|Arteriosclerosis|Cardiovascular Diseases|Heart Diseases|Vascular Diseases Keimyung University Dongsan Medical Center May 2016 --
NCT02452736 Completed Ischemic Heart Disease|Cardiovascular Diseases|Arteriosclerosis|Coronary Artery Disease Medtronic Vascular May 2015 Phase 3
NCT02360423 Recruiting Coronary Artery Disease CID S.p.A. November 2014 Phase 3
NCT02098876 Recruiting Coronary Artery Disease Emory University|Medtronic May 2014 Phase 4
NCT01397175 Active, not recruiting Coronary Artery Disease Yonsei University|Gangwon Cardiovascular Health Research Institute January 2013 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID