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Zotarolimus

Catalog No. T6033   CAS 221877-54-9
Synonyms: ABT-578, A 179578

Zotarolimus (ABT-578), an analogue of rapamycin, inhibits FKBP-12 (IC50= 2.8 nM).

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Zotarolimus Chemical Structure
Zotarolimus, CAS 221877-54-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 60.00
2 mg In stock $ 88.00
5 mg In stock $ 147.00
10 mg In stock $ 237.00
25 mg In stock $ 413.00
50 mg In stock $ 595.00
100 mg In stock $ 862.00
1 mL * 10 mM (in DMSO) In stock $ 251.00
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Purity: 95%
Purity: 95%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Zotarolimus (ABT-578), an analogue of rapamycin, inhibits FKBP-12 (IC50= 2.8 nM).
Targets&IC50 FKBP-12:2.8 nM
In vitro In smooth muscle cell (IC50=2.9 nM)and endothelial cell (IC50=2.6 nM),Zotarolimus effectively inhibits cells proliferation.
In vivo Zotarolimus potently inhibits adjuvant DTH(ED50=1.72 mg/kg/day), EAE(ED50=1.17 mg/kg/day), and cardiac allograft rejection(ED50=3.71 mg/kg/day) .
Kinase Assay zotarolimus (10 pM-1 μM) in buffer A (2% BSA and 0.2% Tween-20 in D-PBS) is used in the assay of Binding Affinity to FKBP12.
Cell Research 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 Male Sprague-Dawley rats was administrate by intravenous or oral Zotarolimus(2.5 mg/kg)dissolved inethanol: propylene glycol: cremophor EL: D5W vehicle (20: 30: 2: 48, by volume).
Synonyms ABT-578, A 179578
Molecular Weight 966.21
Formula C52H79N5O12
CAS No. 221877-54-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 93 mg/mL (96.3 mM)

DMSO: 93 mg/mL (96.3 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Garcia-Touchard A, et al. Eur Heart J, 2006, 27(8), 988-1993. 2. Chen YW, et al. J Cardiovasc Pharmacol, 2007, 49(4), 228-235.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library FDA-Approved & Pharmacopeia Drug Library Clinical Compound Library PI3K-AKT-mTOR Compound Library Oxidation-Reduction Compound Library Inhibitor Library Drug Repurposing Compound Library Macrocyclic Compound Library Anti-Ovarian Cancer Compound Library

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Keywords

Zotarolimus 221877-54-9 PI3K/Akt/mTOR signaling mTOR coronary ABT 578 drug-eluting inhibit artery disease ABT-578 restenosis Rapamycin ABT578 immunosuppressant A-179578 stents A179578 Inhibitor A 179578 inhibitor

 

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