Everolimus is an inhibitor of mTOR through binding FKBP12 with IC50 of 1.6-2.4 nM, which also shows inhibition in several hormone therapy–sensitive ERb breast cancer xenograft models like MCF7 and HCC1500, as well as three patient-derived primary explant models BR0555, CTC174, and HBCx3. Up to now, AZD2014 enters Phase 1 trial in solid tumours.
Everolimus/依维莫司 细胞实验
Cell Line
Concentration
Treated Time
Description
References
UM-UC-14 bladder cancer cells
0.1, 0.5, 1, 10, 20, or 100 nM
4 and 6 days
To assess the effect of RAD001 on bladder cancer cell growth. RAD001 inhibited the growth of all bladder cancer cells in a dose-dependent manner.
Clin Cancer Res. 2011 May 1;17(9):2863-73.
UM-UC-9 bladder cancer cells
0.1, 0.5, 1, 10, 20, or 100 nM
4 and 6 days
To assess the effect of RAD001 on bladder cancer cell growth. RAD001 inhibited the growth of all bladder cancer cells in a dose-dependent manner.
Clin Cancer Res. 2011 May 1;17(9):2863-73.
UM-UC-6 bladder cancer cells
0.1, 0.5, 1, 10, 20, or 100 nM
4 and 6 days
To assess the effect of RAD001 on bladder cancer cell growth. RAD001 inhibited the growth of all bladder cancer cells in a dose-dependent manner.
Clin Cancer Res. 2011 May 1;17(9):2863-73.
UM-UC-3 bladder cancer cells
0.1, 0.5, 1, 10, 20, or 100 nM
4 and 6 days
To assess the effect of RAD001 on bladder cancer cell growth. RAD001 inhibited the growth of all bladder cancer cells in a dose-dependent manner.
Clin Cancer Res. 2011 May 1;17(9):2863-73.
T47D
100 nM
6-12 months
Generate Everolimus-resistant cell lines and confirm their resistance
Elife. 2023 Sep 29;12:e85898.
MCF7
100 nM
6-12 months
Generate Everolimus-resistant cell lines and confirm their resistance
Elife. 2023 Sep 29;12:e85898.
CAMA-1
50 nM
6-12 months
Generate Everolimus-resistant cell lines and confirm their resistance
Elife. 2023 Sep 29;12:e85898.
LoVo cells
10 nM, 100 nM, 1 µM
72 h
To evaluate the effects of Everolimus on cell cycle, cell death, and autophagy in LoVo cells. Results showed that Everolimus had minor effects on LoVo cells.
Cell Death Dis. 2021 Oct 21;12(11):978.
MDST8 cells
10 nM, 100 nM, 1 µM
72 h
To evaluate the effects of Everolimus on cell cycle, cell death, and autophagy in MDST8 cells. Results showed that Everolimus significantly inhibited MDST8 cell growth, induced cell cycle arrest, and autophagy.
Cell Death Dis. 2021 Oct 21;12(11):978.
Everolimus/依维莫司 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
Subcutaneous tumor model implanted with UM-UC-3, UM-UC-6, and UM-UC-9 cells
Oral gavage
5 mg/kg
Twice weekly for 1 month
To evaluate the effect of RAD001 on tumor growth in vivo. RAD001 significantly inhibited the growth of tumors subcutaneously implanted in mice.
Clin Cancer Res. 2011 May 1;17(9):2863-73.
Nude mice
MDST8 tumor model
Intraperitoneal injection
4 mg/kg
Biweekly for 3 months
To evaluate the therapeutic effects of Everolimus on MDST8 tumors. Results showed that Everolimus significantly reduced MDST8 tumor volume and extended the lifespan of mice.
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