体外研究 (In Vitro) |
ATX inhibitor 13 (compound 10c) (0-20 μM, 72 h) shows cytotoxicity and anti-proliferative activity against MCF-7, MDA-MB-231, A549, NCI-H1581, H2228, Hep3B, and RAW264.7 cells[1]. ATX inhibitor 13 (0-1 μM, 0-72 h) inhibits migration of RAW264.7 cells in a dose-dependent manner, significantly down-regulates both the colony count and colony single area with the concentration elevation[1]. ATX inhibitor 13 (0-1 μM, 72 h) dose dependently suppresses colony formation of RAW264.7 cells[1]. ATX inhibitor 13 (0-1 μM, 48 h) induces weak apoptosis in a dose-dependent manner in RAW264.7 cells[1]. ATX inhibitor 13 (0-1 μM, 48 h) brings G2 phase arrest of RAW264.7 cells[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay
Cell Line: |
MCF-7, MDA-MB-231, A549, NCI-H1581, H2228, Hep3B, RAW264.7[1] |
Concentration: |
0-20 μM |
Incubation Time: |
72 h |
Result: |
Showed cytotoxicity and antiproliferative activity against MCF-7, MDA-MB-231, A549, NCI-H1581, H2228, Hep3B, and RAW264.7 cell lines, with IC50 values of 3.87 ± 0.37, 3.29 ± 0.37, 6.59 ± 0.26, 4.76 ± 0.57, 4.27 ± 0.21, 0.58 ± 0.11, and 0.63 ± 0.26 μM. |
Apoptosis Analysis
Cell Line: |
RAW264.7 cells[1] |
Concentration: |
0 μM, 0.1 μM, 0.25 μM, 0.5 μM and 1 μM |
Incubation Time: |
48 h |
Result: |
Induced apoptosis in a dose-dependent manner, with the apoptotic rates of 6.48% (0.1 μM), 7.73% (0.25 μM), 8.60% (0.5 μM) and 9.17% (1 μM). |
Cell Cycle Analysis
Cell Line: |
RAW264.7 cells[1] |
Concentration: |
0 μM, 0.1 μM, 0.25 μM, 0.5 μM and 1 μM |
Incubation Time: |
24 h |
Result: |
Led to significant G2 phase arrest in RAW264.7 cells in a dose-dependent manner, the percentage of cells in the G2 phase slightly increased from 10.90% to 90.16% (0-1 μM). |
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体内研究 (In Vivo) |
ATX inhibitor 13 (compound 10c) (C57BL/6J mice, 0-1000 mg/kg, Orally, once) has an acceptable safety profile[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: |
C57BL/6J mice (5 groups,4 mice per group)[1] |
Dosage: |
5000, 3200, 2500 and 1000 mg/kg |
Administration: |
Orally, once |
Result: |
Had an acceptable safety profile, showed no obvious safety concerns. |
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