Mito-TP-2

Mito-TP-2 is a triptolide derivative. Mito-TP-2 exhibits concentration-dependent cytotoxicity in cancer cells. Mito-TP-2 is selectively driven and accumulated into the mitochondria of tumor cells by mitochondrial transmembrane potential and exerts specific mitochondrial toxicity. Mito-TP-2 can be used for the research of liver cancer, breast cancer, and non-small cell lung cancer ^{[1] [2] [3]}.

In Vitro, Mito-TP-2 (48 h) potently inhibits HepG-2 human hepatocellular carcinoma cells (IC₅₀=0.067 μM) and MCF-7 human breast cancer cells (IC₅₀=0.238 μM), while showing 16-fold reduced toxicity to L-02 human normal hepatocytes (IC₅₀=0.334 μM) compared to Triptolide ^[1]. Mito-TP-2 (48 h) potently inhibits NCI-H1975 cell proliferation with an IC₅₀ of 0.14 μM, while showing minimal activity against BEAS-2B, MCF-7, A549, and NCI-H460 cells^[2]. Mito-TP-2 accumulates to a higher level than Triptolide in HepG2 cell mitochondria, shows enhanced antitumor selectivity, and exhibits reduced toxicity toward normal cells^[3].

References:
[1]. Fan P, et al. Triptolide derivative and preparation method and application thereof. China, CN111518157A. 2020-08-11.
[2]. Xing W, et al. Selective Antitumor Effect and Lower Toxicity of Mitochondrion-Targeting Derivatization of Triptolide. J Med Chem. 2024;67(2):1093-1114.
[3]. Zhang X, et al. Pro-drug approaches to overcome poor solubility and toxicity of triptolide. Phytochemistry Reviews. 2025 Aug 06;25:1565-1580.