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500mg |
ln Vitro |
Tigecycline (0.63-30 µM, administered for 72 hours after pre-incubation for 4 days) inhibits HL-60 cells and AML2 cells, with freshly generated IC50 values of 3.06±0.85 μM and 4.72±0.54 μM, respectively. After one day of pre-incubation, tigecycline inhibits HL-60 cells and AML2 cells with IC50 values of 4.27±0.45 μM and 5.64±0.55 μM, respectively. After two days of pre-incubation, tigecycline inhibits AML2 cells and HL-60 cells with IC50 values of 5.02±0.60 and 4.39±0.44 μM, respectively. After three days of pre-incubation, tigecycline inhibits HL-60 cells and AML2 cells with IC50 values of 3.95±0.39 μM and 4.09±0.41 μM, respectively. The CellTiter Flour test revealed that tigecycline's capacity to kill TEX human leukemia cells decreased after 4 days of pre-incubation in saline (from IC50~5 µM when freshly prepared to IC50> after 4 days of pre-incubation 50 µM) [1].
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ln Vivo |
In NOD/SCID mice, tigecycline (50 mg/kg; i.p.; twice daily; for 11 days) decreases tumor weight and volume [1]. The results showed that the replacement time was 108.9 minutes, and the peak plasma concentration (Cmax), terminal half-life (t1/2), area under the plasma concentration-time curve (AUC), clearance (CL), and distribution volume (Vz) were all 22.8 μg/mL. In saline, the gacycline concentrations were 1912.2min*μg/mL, 26.1 mL/min/kg, and 4109.4 mL/kg, in that order. The following values were obtained during the preparation process: 15.7 μg/mL for the peak plasma concentration (Cmax), t1/2 for the terminal half-life, AUC for the area under the plasma concentration-time curve, CL for clearance, and Vz for volume of distribution. The concentrations of tigecycline were 2036.5 min*μg/mL, 24.6 mL/min/kg, and 3906.2 mL/kg (60 mg/mL pyruvate, 3 mg/mL ascorbic acid, pH 7, in saline) [1].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: Human Leukemia OCI-AML2, HL-60 (ATCC) and TEX Cell Lines Tested Concentrations: 0.63-30 µM Incubation Duration: 4 days of pre-incubation, 72 hrs (hours) of treatment Experimental Results: Inhibition of AML2 cells and HL - 60 cells, IC50 is 4.72±0.54 and 3.06±0.85 μM (freshly prepared). |
Animal Protocol |
Animal/Disease Models: NOD/SCID mouse OCI-AML2 acute myeloid leukemia (AML) xenograft model [1]
Doses: 50 mg/kg Route of Administration: intraperitoneal (ip) injection; twice (two times) daily; for 11 days Experimental Results: Tumor volume and weight decrease. Animal/Disease Models: NOD/SCID (severe combined immunodeficient) mouse[1] Doses: 50 mg/kg Route of Administration: intraperitoneal (ip) injection; 360 minutes Experimental Results: peak plasma concentration (Cmax), terminal half-life (t1/2), plasma concentration-time The area under the curve (AUC), clearance (CL) and distribution volume (Vz) were all 22.8 μg/108.9 minutes, 1912.2 minutes*μg/ml, 26.1 ml/minute/kg, and 4109.4 ml/kg respectively. |
References |
[1]. Jitkova Y, et al. A novel formulation of tigecycline has enhanced stability and sustained antibacterial and antileukemic activity. PLoS One. 2014 May 28;9(5):e95281.
[2]. Falagas ME, et al. Activity of TP-6076 against carbapenem-resistant Acinetobacter baumannii isolates collected from inpatients in Greek hospitals. Int J Antimicrob Agents. 2018 Aug;52(2):269-271. |
Molecular Formula |
C30H43N5O11S
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Molecular Weight |
681.7543
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CAS # |
1135871-27-0
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Related CAS # |
Tigecycline;220620-09-7;Tigecycline tetramesylate;Tigecycline hydrochloride;197654-04-9;Tigecycline hydrate;1229002-07-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
S(C([H])([H])[H])(=O)(=O)O[H].O([H])[C@@]12C(=C(C(N([H])[H])=O)C([C@]([H])([C@]1([H])C([H])([H])[C@]1([H])C([H])([H])C3=C(C([H])=C(C(=C3C(=C1C2=O)O[H])O[H])N([H])C(C([H])([H])N([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])=O)N(C([H])([H])[H])C([H])([H])[H])N(C([H])([H])[H])C([H])([H])[H])=O)O[H]
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.4668 mL | 7.3341 mL | 14.6681 mL | |
5 mM | 0.2934 mL | 1.4668 mL | 2.9336 mL | |
10 mM | 0.1467 mL | 0.7334 mL | 1.4668 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.