PTC-209 is a specific inhibitor for BMI-1 with IC50 of 0.5 μM in in both GEMS reporter and ELISA assays.
PTC-209 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Cal27 cells
10 µM
48 hours
PTC-209 significantly inhibited cell proliferation and induced G1-phase cell cycle arrest and apoptosis
Cancer Cell Int. 2017 Nov 21;17:107.
FaDu cells
10 µM
48 hours
PTC-209 significantly inhibited cell proliferation and induced G1-phase cell cycle arrest and apoptosis
Cancer Cell Int. 2017 Nov 21;17:107.
CP20 cells
100 nM
48 hours
PTC-209 significantly increased LC3B-II and reduced SQSTM1 and BMI1 levels, indicating induction of autophagy
Autophagy. 2016;12(4):659-70.
OVCAR4 cells
100 nM
48 hours
PTC-209 significantly increased LC3B-II and reduced SQSTM1 and BMI1 levels, indicating induction of autophagy
Autophagy. 2016;12(4):659-70.
ATRT-like cells
100, 50, 10, 5, 6.25, 1, 0.5, 0.1, 0.05, 0.01 µM
48 hours
To test the effect of PTC-209 on the viability of ATRT-like cells, results showed that PTC-209 significantly reduced cell viability.
Bioact Mater. 2023 Aug 12;31:136-150.
HCT116 cells
1.67 µM
72 hours
PTC-209 showed anti-proliferative activity in HCT116 cells with an IC50 of 1.67 μM.
J Exp Clin Cancer Res. 2019 Oct 22;38(1):422.
HT29 cells
1.36 µM
72 hours
PTC-209 showed anti-proliferative activity in HT29 cells with an IC50 of 1.36 μM.
J Exp Clin Cancer Res. 2019 Oct 22;38(1):422.
Human multiple myeloma cell lines (HMCLs)
0.01 –10 µM
96 hours
PTC-209 significantly decreased the viability of all analysed human multiple myeloma cell lines with IC50 values <2 μM in six of eight HMCLs, and IC50 values were not reached in healthy donor peripheral blood mononuclear cells (PBMCs) and bone marrow stromal cells (BMSCs).
J Hematol Oncol. 2016 Mar 2;9:17.
Human bone marrow stromal cells (BMSCs)
0.01 –10 µM
96 hours
PTC-209 did not reach IC50 values in healthy donor peripheral blood mononuclear cells (PBMCs) and bone marrow stromal cells (BMSCs), indicating lower toxicity to normal cells.
J Hematol Oncol. 2016 Mar 2;9:17.
PTC-209 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
HNSCC xenograft model
Subcutaneous injection
30 mg/kg
Daily for 15 consecutive days
PTC-209 significantly inhibited tumor growth, likely through Bmi1 inhibition and impaired cell proliferation
Cancer Cell Int. 2017 Nov 21;17:107.
BALB/c Nude mice
Subcutaneous tumor xenograft model
Intraperitoneal injection
30 mg/kg
Once daily for 24 days
PTC-209 significantly inhibited subcutaneous tumor growth with no obvious toxicity.
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