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CTPI-2 is a selective mitochondrial citrate transporter (SLC25A1) inhibitor that displays H1299 anti-proliferation activity in a SLC25A1-dependent manner (IC50 <10 μM). When compared with CTPI-1, CTPI-2 exhibits 20-fold higher target affinity (hSLC25A1 KD = 3.5 μM vs. 63.6 μM, respectively) and is ~1000-fold more potent against H1299 sphere-forming capacity. CTPI-2 inhibits mitochondrial respiration and formation of patient NSCLC tumors-derived CSCs spheres in cultures (10-50 μM), as well as suppresses the growth of patent-derived NSCLC exnografts in mice in vivo (28 mg/kg q.o.d. i.p.).
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Cell death and differentiation, 25(7), 1239-1258 (2018-04-14)
Therapy resistance represents a clinical challenge for advanced non-small cell lung cancer (NSCLC), which still remains an incurable disease. There is growing evidence that cancer-initiating or cancer stem cells (CSCs) provide a reservoir of slow-growing dormant populations of cells with
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