1135871-27-0
1135871-27-0 用途与合成方法
Mean MIC: 125 ng/mL (
E. coli
)
MIC50: 1 mg/mL (
A. baumannii
)
MIC90: 2 mg/mL (
A. baumannii
)
Tigecycline (0.63-30 µM, preincubated for 4 days, treated for 72 h) inhibits AML2 cells and HL-60 cells with IC 50 s of 4.72±0.54 and 3.06±0.85 μM (freshly prepared). Tigecycline inhibits AML2 cells and HL-60 cells with IC 50 s of 5.64±0.55 and 4.27±0.45 μM (1 day preincubation). Tigecycline inhibits AML2 cells and HL-60 cells with IC 50 s of 5.02±0.60 and 4.39±0.44 μM (2 day preincubation). Tigecycline inhibits AML2 cells and HL-60 cells with IC 50 s of 4.09±0.41 and 3.95±0.39 μM (3 day preincubation). After a 4 day preincubation of Tigecycline in saline, Tigecycline lost its ability to kill TEX human leukemia cells (from IC 50 ~5 µM when freshly prepared to IC 50 >50 µM after 4 days preincubation) as measured by CellTiter Flour assay.
Cell Viability Assay
| Cell Line: | Human leukemic OCI-AML2, HL-60 (ATCC) and TEX cell lines |
| Concentration: | 0.63-30 µM |
| Incubation Time: | Preincubated for 4 days, treated for 72 hours |
| Result: | Inhibited AML2 cells and HL-60 cells with IC 50 s of 4.72±0.54 and 3.06±0.85 μM (freshly prepared). |
Tigecycline (50 mg/kg; intraperitoneal injection; twice a day; for 11 days) reduces tumor volume and weight in NOD/SCID mice.
The peak plasma concentration (C
max
), the terminal half-life (t
1/2
), area under the plasma concentration-time curve (AUC), clearance (CL) and volume of distribution (Vz) are 22.8μg/mL, 108.9 min, 1912.2min*μg/mL, 26.1 mL/min/kg, 4109.4 mL/kg for Tigecycline in saline, respectively. The peak plasma concentration (C
max
), the terminal half-life (t
1/2
), area under the plasma concentration-time curve (AUC), clearance (CL) and volume of distribution (Vz) are15.7μg/mL, 110.3 min, 2036.5 min*μg/mL, 24.6 mL/min/kg, 3906.2 mL/kg for Tigecycline in formulation (60 mg/mL pyruvate, 3 mg/mL ascorbic acid, pH 7 in saline) , respectively.
| Animal Model: | NOD/SCID mice with OCI-AML2 acute myeloid leukemia (AML) xenograft model |
| Dosage: | 50 mg/kg |
| Administration: | Intraperitoneal injection; twice a day; for 11 days |
| Result: | Reduced tumor volume and weight. |
| Animal Model: | NOD/SCID mice |
| Dosage: | 50 mg/kg |
| Administration: | Intraperitoneal injection; 360 minutes |
| Result: | The peak plasma concentration (C max ), the terminal half-life (t 1/2 ), area under the plasma concentration-time curve (AUC), clearance (CL) and volume of distribution (Vz) are 22.8 μg/mL, 108.9 min, 1912.2 min*μg/mL, 26.1 mL/min/kg, 4109.4 mL/kg, respectively. |
