The mutant IDH1 inhibitor is highly effective against IDH1 R132H and is employed in the treatment of diseases or conditions linked to this mutant IDH protein, including but not limited to cell-proliferation disorders such as cancer [1].
体外研究
The mutant IDH1 inhibitor is highly effective against IDH1 R132H and is employed in the treatment of diseases or conditions linked to this mutant IDH protein, including but not limited to cell-proliferation disorders such as cancer [1].
Mutant IDH1 inhibitor 细胞实验
Cell Line
Concentration
Treated Time
Description
References
TF-1 cells
500 nM
To assess the transforming ability of IDH1 R132H/D279N double mutant in TF-1 cells and its sensitivity to ivosidenib. Results showed that IDH1 R132H/D279N could induce cytokine-independent proliferation in TF-1 cells and was resistant to ivosidenib.
NPJ Precis Oncol. 2022 Sep 2;6(1):61.
Human chondrosarcoma cells
82.5 μM
4 days
To evaluate the effect of CP-91149 on cell apoptosis, results showed increased TUNEL-positive cells, indicating increased apoptosis.
Cell Rep. 2023 Jun 27;42(6):112578.
Human chondrosarcoma cells
82.5 μM
18 h
To evaluate the effect of CP-91149 on cell proliferation, results showed reduced BrdU incorporation, indicating inhibition of cell proliferation.
Cell Rep. 2023 Jun 27;42(6):112578.
Human chondrosarcoma cells
82.5 μM
96 h
To evaluate the effect of CP-91149 on cell viability, results showed significant reduction in cell viability.
Cell Rep. 2023 Jun 27;42(6):112578.
Mutant IDH1 inhibitor 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Patient-derived xenograft model
Intraperitoneal injection
50 mg/kg
5 days a week for 2 weeks
To evaluate the effect of CP-91149 on tumor growth, results showed significant reduction in tumor size, tumor weight, and tumor volume, and reduced BrdU incorporation, indicating inhibition of cell proliferation.
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