- Tandutinib (MLN518/CT53518) targeted to stem-like cells by inhibiting the function of ATP-binding cassette subfamily G member 2.
Tandutinib (MLN518/CT53518) targeted to stem-like cells by inhibiting the function of ATP-binding cassette subfamily G member 2.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences (2013-04-27)
Xiao-qin Zhao, Chun-ling Dai, Shinobu Ohnuma, Yong-ju Liang, Wen Deng, Jun-Jiang Chen, Mu-Sheng Zeng, Suresh V Ambudkar, Zhe-Sheng Chen, Li-Wu Fu
PMID23619284
ABSTRAKT
Tandutinib is a novel inhibitor of tyrosine kinases FLT3, PDGFR and KIT. Our study was to explore the capability of tandutinib to reverse ABC transporter-mediated multidrug resistance. Tandutinib reversed ABCG2-mediated drug resistance in ABCG2-482-R2, ABCG2-482-G2, ABCG2-482-T7 and S1-M1-80 cells and increased the accumulation of doxorubicin, rhodamine 123 and [H(3)] mitoxantrone in ABCG2-overexpressing cells. Importantly, tandutinib selectively sensitized side population cells to mitoxantrone. Taken together, our results advocate the potency of tandutinib as an ABCG2 modulator and stem-like cells targeted agent to increase efficiency of anticancer drugs.
MATERIAŁY