生物活性 | |||
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描述 | Leukemia inhibitory factor (LIF) is a pleiotropic cytokine that belongs to the interleukin-6 family. The overexpression of LIF is associated with tumor growth and low relapse-free survival rate. EC330 is a novel, orally bioavailable, steroidal LIF inhibitor that shows cytotoxicity in NCI-60 cell line panel and different types of cancer cell lines at low nanomolar concentration. It also blocked the colony formation and angiogenesis in HUVEC cells. EC330 demonstrated higher specificity in LIF-overexpressing MCF-7 cells versus wild-type MCF-7 cells. It disrupted cytoskeleton and targeted cancer-associated fibroblasts via the inhibition of alpha-SMA. In xenograft mouse models of ovarian (IGROV-1) and triple negative breast cancer (MDA-MB-231) cells, as well as the model of MDA-MB-231 patient-derived xenograft, treatment with EC330 at 0.1, 0.5 and 2.5mg/kg decreased tumor burden at a dose-dependent manner compared to the control group[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.16mL 0.43mL 0.22mL |
10.81mL 2.16mL 1.08mL |
21.62mL 4.32mL 2.16mL |
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