Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Zotarolimus (ABT-578), an analogue of rapamycin, inhibits FKBP-12 (IC50= 2.8 nM).
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 93 mg/mL (96.3 mM)
DMSO: 93 mg/mL (96.3 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
You can also refer to dose conversion for different animals. More
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