GLPBio

Zotarolimus(ABT-578)

Catalog No.: GC14224Purity:>98.50%Synonyms: A-179578, ABT-578
COASDSData Sheet
Zotarolimus(ABT-578) is an immunosuppressant that inhibits immunophilin FKBP12 binding with an IC50 of 2.8±0.16nM.

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Zotarolimus(ABT-578)
Cas No.: 221877-54-9
1mgIn Stock
$35.00
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5mgIn Stock
$77.00
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10mgIn Stock
$129.00
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25mgIn Stock
$245.00
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Description

Zotarolimus(ABT-578) is an immunosuppressant that inhibits immunophilin FKBP12 binding with an IC50 of 2.8±0.16nM[1]. Zotarolimus binds to the immunoaffinity protein FKBP12 to form the Zotarolimus-FKBP12 complex, which inhibits mammalian target of rapamycin (mTOR) to regulate intracellular metabolism[2]. Zotarolimus has been widely used in the development of novel drug-eluting stents to prevent coronary restenosis[3].

In vitro, Zotarolimus treatment for 48h inhibited human coronary artery smooth muscle cell (HCASMC) proliferation, with an IC50 value of 0.8nM[4]. Treatment with 1µM Zotarolimus for 48 hours significantly inhibited the migration of human coronary artery endothelial cells (HCAECs) and reduced the expression of pro-inflammatory cytokines[5].

In vivo, Zotarolimus treatment via intraperitoneal injection at a dose of 2mg/kg/day for 3 weeks suppressed tumor growth in the HCT-116 cell xenograft tumor mouse model[6]. Combined administration of Zotarolimus (2mg/kg/day) and 5-fluorouracil (100mg/kg/week) by intraperitoneal injection for 3 weeks significantly inhibited the progression of lung adenocarcinoma in the A549 cell xenograft mouse model and suppressed the expression of IL-1β and TNF-α[7].

References:
[1] Garcia-Touchard A, Burke S E, Toner J L, et al. Zotarolimus-eluting stents reduce experimental coronary artery neointimal hyperplasia after 4 weeks[J]. European heart journal, 2006, 27(8): 988-993.
[2] Shokati T, Drake S H, Zhao W, et al. Structural Identification of Zotarolimus (ABT-578) Metabolites Generated by Human Liver Microsomes Using Ion-Trap and High-Resolution Time-of-Flight Mass Spectrometry in Combination with the Analysis of Fragmentation Patterns[J]. Metabolites, 2023, 13(10): 1093.
[3] Burke S E, Kuntz R E, Schwartz L B. Zotarolimus (ABT-578) eluting stents[J]. Advanced drug delivery reviews, 2006, 58(3): 437-446.
[4] Chen Y W, Smith M L, Sheets M, et al. Zotarolimus, a novel sirolimus analogue with potent anti-proliferative activity on coronary smooth muscle cells and reduced potential for systemic immunosuppression[J]. Journal of cardiovascular pharmacology, 2007, 49(4): 228-235.
[5] Steinfeld D S, Liu A P, Hsu S H, et al. Comparative assessment of transient exposure of paclitaxel or zotarolimus on in vitro vascular cell death, proliferation, migration, and proinflammatory biomarker expression[J]. Journal of Cardiovascular Pharmacology, 2012, 60(2): 179-186.
[6] Chang G R, Kuo C Y, Tsai M Y, et al. Anti-cancer effects of zotarolimus combined with 5-fluorouracil treatment in HCT-116 colorectal cancer-bearing BALB/c nude mice[J]. Molecules, 2021, 26(15): 4683.
[7] Wu C F, Wu C Y, Chiou R Y Y, et al. The anti-cancer effects of a zotarolimus and 5-fluorouracil combination treatment on A549 cell-derived tumors in Balb/c nude mice[J]. International Journal of Molecular Sciences, 2021, 22(9): 4562.

Protocol

Cell experiment [1]:

Cell lines

Human coronary artery smooth muscle cell (HCASMC)

Preparation Method

HCASMCs were cultured in SmGM-2 growth media, containing fetal bovine serum (5%) and a specific cocktail of growth factors and antibiotics. All cells were cultured in a 37ºC and 5% CO2 environment, and refed every 3–4 days or passed on reaching 80% confluence. HCASMCs were seeded at a density optimal for growth (1.5×104 cells per centimeter square) in black-walled 96-well plates. Proliferation of HCASMCs under constant exposure to Zotarolimus over a range of concentrations (0.00001, 0.0001, 0.001, 0.01, 0.1, and 1µM) and over a period of 48 hours was observed using the pico green dye assay used for evaluation.

Reaction Conditions

0.00001, 0.0001, 0.001, 0.01, 0.1, and 1µM; 48h

Applications

Zotarolimus treatment significantly reduced the viability of HCASMCs in a dose-dependent manner.
Animal experiment [2]:

Animal models

Male BALB/c nude mice

Preparation Method

Six weeks old male BALB/c nude mice were maintained in a constant temperature (22±2°C) and constant humidity (55±5%) environment with a light/dark cycle of 12h/12h. After the mice were anesthetized by intraperitoneal injection of Zoletil, 100µl HCT-116 cell suspension containing 1×106 live HCT-116 cells was injected subcutaneously into the hind limbs. After 7 days of continuous feeding, the mice with tumors of 4-5mm in diameter were divided into 3 groups. Tumor growth was analyzed after three weeks of intraperitoneal injection of 5-fluorouracil (5-FU; 50mg/kg/week) and Zotarolimus (2mg/kg/day) in the second and third groups, respectively. After three weeks, tumor growth was analyzed.

Dosage form

2mg/kg/day for 3 weeks; i.p.

Applications

Zotarolimus treatment suppressed tumor growth in HCT-116 cell xenograft tumor mouse model.

References:
[1] Steinfeld D S, Liu A P, Hsu S H, et al. Comparative assessment of transient exposure of paclitaxel or zotarolimus on in vitro vascular cell death, proliferation, migration, and proinflammatory biomarker expression[J]. Journal of Cardiovascular Pharmacology, 2012, 60(2): 179-186.
[2] Chang G R, Kuo C Y, Tsai M Y, et al. Anti-cancer effects of zotarolimus combined with 5-fluorouracil treatment in HCT-116 colorectal cancer-bearing BALB/c nude mice[J]. Molecules, 2021, 26(15): 4683.

Product Documents

Purity:>98.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
221877-54-9
Synonyms
A-179578, ABT-578
Molecular Formula
C52H79N5O12
Molecular Weight
966.21
Solubility
DMF: 15mg/mL,DMSO: 15mg/mL,Ethanol: 20mg/mL,Ethanol:PBS (pH 7.2) (1:3): 0.25mg/mL
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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