Eribulin mesylate, at concentrations ranging from 1 to 100 nM over 72 hours, inhibits cell proliferation with IC50 values of 22.8 nM for LM8 cells and 21.5 nM for Dunn cells[1]. Eribulin mesylate (1-100 nM; 72 h) inhibits cell proliferation with IC50 values of 22.8 nM for LM8 cells and 21.5 nM for Dunn cells[1]. Eribulin mesylate (10-50 nM; 12-72 h) induces G2/M arrest in LM8 cells within 12 hours at a concentration of 50 nM. However, this effect is not observed with a longer treatment duration of 72 hours at 10 nM[1]. Eribulin mesylate, at concentrations from 1 to 50 nM over 12 hours, does not induce senescence in LM8 cells[1]. Eribulin mesylate (1-10 nM; 16 h) induces morphological changes and suppresses cell migration in LM8 cells[1].
体内研究
Eribulin mesylate (1 mg/kg; i.v. once a week for 2 weeks) reduces primary tumor growth and lung metastasis in a mouse model of osteosarcoma[1].
Eribulin mesylate (1 mg/kg; once i.v.) suppresses the appearance of circulating tumor cells (CTC) during the low-concentration phase[1].
体外研究
Eribulin mesylate, at concentrations ranging from 1 to 100 nM over 72 hours, inhibits cell proliferation with IC50 values of 22.8 nM for LM8 cells and 21.5 nM for Dunn cells[1].
Eribulin mesylate (1-100 nM; 72 h) inhibits cell proliferation with IC50 values of 22.8 nM for LM8 cells and 21.5 nM for Dunn cells[1].
Eribulin mesylate (10-50 nM; 12-72 h) induces G2/M arrest in LM8 cells within 12 hours at a concentration of 50 nM. However, this effect is not observed with a longer treatment duration of 72 hours at 10 nM[1].
Eribulin mesylate, at concentrations from 1 to 50 nM over 12 hours, does not induce senescence in LM8 cells[1].
Eribulin mesylate (1-10 nM; 16 h) induces morphological changes and suppresses cell migration in LM8 cells[1].
Eribulin Mesylate/甲磺酸艾日布林 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Hs578T cells
1 nM
72 hours
To evaluate the effect of eribulin on cell viability, results showed that eribulin reduced cell viability in a dose-dependent manner.
Cell Mol Life Sci. 2024 Dec 31;82(1):32
MDA-MB-231 cells
1.2 nM and 2.4 nM
72 hours
To evaluate the effect of eribulin on cell viability, results showed that eribulin reduced cell viability in a dose-dependent manner.
Cell Mol Life Sci. 2024 Dec 31;82(1):32
HER2-negative breast cancer cell lines
0.25 nM
Evaluate the antiproliferative activity of eribulin, results showed PIK3CA-mutant cells were resistant to eribulin
Br J Cancer. 2021 Apr;124(9):1581-1591
MCF10A PIK3CA-wt/p.H1047R
1 nM
1 week
Evaluate the antiproliferative activity of eribulin, results showed PIK3CA-wt/p.H1047R cells were resistant to eribulin
Br J Cancer. 2021 Apr;124(9):1581-1591
MCF10A PIK3CA-wt/wt
1 nM
1 week
Evaluate the antiproliferative activity of eribulin, results showed PIK3CA-wt/wt cells were sensitive to eribulin
Br J Cancer. 2021 Apr;124(9):1581-1591
ES-4 cells
0.01 – 0.1 nM
72 hours
To evaluate the cytotoxic effects of eribulin combined with SN-38 (active metabolite of irinotecan) in vitro. Results showed that the combination of eribulin and SN-38 exhibited additive effects at most concentration pairs, but showed synergy at low concentrations (0.01 – 0.1 nM).
Clin Cancer Res. 2020 Jun 15;26(12):3012-3023
SK-UT1-B cells
0.004 to 2µM
72 hours
Evaluate the effect of Eribulin Mesylate combined with selinexor, showing no synergistic effect in SK-UT1-B cells.
Exp Hematol Oncol. 2023 Sep 15;12(1):78
SK-UT1 cells
0.004 to 2µM
72 hours
Evaluate the synergistic effect of Eribulin Mesylate combined with selinexor, showing synergistic anti-tumor effects in SK-UT1 cells.
Exp Hematol Oncol. 2023 Sep 15;12(1):78
PB3 cells
300 nM
4 hours
To evaluate the thermal stability effects of Eribulin on PB3 cells, it was found that Eribulin altered the thermal stability of SMARCD1 and SMARCD3.
Cell Rep Med. 2024 Apr 16;5(4):101504
Eribulin Mesylate/甲磺酸艾日布林 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c nude mice
Xenograft model
Intravenous and intraperitoneal injection
0.1 mg/kg
Eribulin every 2 days for 14 days, tubacin daily for 26 days, CCT020312 every 4 days for 26 days
To evaluate the effect of combined treatment with eribulin, tubacin, and CCT020312 on the growth of EriR xenograft tumors, results showed that the combined treatment significantly inhibited tumor growth.
Cell Mol Life Sci. 2024 Dec 31;82(1):32
Nude mice
HER2-negative breast cancer xenograft models
Intravenously
0.1 mg/kg
Weekly on days 1, 3, 5
Evaluate the antitumor activity of eribulin in HER2-negative breast cancer xenograft models, results showed PIK3CA/AKT1 mutations were associated with eribulin resistance
Br J Cancer. 2021 Apr;124(9):1581-1591
C.B.17SC scid−/− female mice
12 xenograft models (9 PDX, 3 CDX)
Intraperitoneal injection
1 mg/kg
Eribulin was administered on days 1 and 8, irinotecan on days 1–5, with the cycle repeated every 21 days.
To evaluate the efficacy of eribulin combined with irinotecan in pediatric cancer xenograft models. Results showed that the eribulin-irinotecan combination was more effective than vincristine-irinotecan in 6/12 models, significantly activating the TP53 pathway and leading to rapid cell death.
Clin Cancer Res. 2020 Jun 15;26(12):3012-3023
Nude mice
SK-UT1 xenograft model
1 mg/kg
32 days
Evaluate the in vivo anti-tumor effect of Eribulin Mesylate combined with selinexor, showing significant tumor growth inhibition and reduced expression of XPO1 and Ki67.
Exp Hematol Oncol. 2023 Sep 15;12(1):78
Mice
MMTV-PyMT transgenic mice
Intraperitoneal injection
1.6 mg/kg
Twice per week for 2 weeks
To evaluate the effects of Eribulin on tumor growth and metastasis, it was found that Eribulin significantly inhibited tumor growth and lung metastasis.
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