包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
25mg | 电议 |
100mg | 电议 |
Cell lines | DU-145 cell lines |
Preparation Method | DU145 cells were labeled with carboxyfluorescein succinimidyl ester (CFSE) (1μM) and incubated for 20 min at 37℃ protecting from light. After two washes in PBS (37℃), the cells were treated with 2.5 mg/ml of Cabozantinib(XL184). |
Reaction Conditions | 2.5 mg/ml, 48h |
Applications | DU-145 cell lines expressed MET, and Cabozantinib(XL184) treatment had a cytostatic effect, blocking cells in G1 phase. Cabozantinib(XL184) induced an inhibition of the autophagic pathway in DU-145 cells, through an upregulation of the mTOR complex. This may be related to the high expression of the AXL that is observed in DU-145; this is also an RTK target for Cabozantinib(XL184). |
Animal models | 6- to 8-week-old NOD-SCID male mice |
Dosage form | 30 mg/kg/day, oral gavage |
Applications | The expression of matrix metalloproteinase-1 (MMP-1), a crucial factor in cell migration, was markedly decreased in the cabozantinib(XL 184)-treated mice compared to in the vehicle group (P |
产品描述 | Cabozantinib (XL184,BMS-907351) is a novel MET and VEGFR2 inhibitor that simultaneously inhibits metastasis, angiogenesis and tumor growth[1]. Its IC50 values for VEGFR2 and c-Met are 0.035 nM and 1.3 nM[2]. Cabozantinib(XL184) treatment of MAME cultures of MDA-MB-231 and HCC70 cells (HGF-expressing fibroblasts) was cytotoxic and significantly reduced multicellular invasive outgrowths, even in cultures with HGF-expressing fibroblasts[3]. The cellular stress induced by Cabozantinib resulted in the induction of ICD (a peculiar type of apoptosis) in DU-145 cell line[4]. Cabozantinib has been reported to inhibit MMP-1 expression by blocking the HGF-MET signaling pathway in bladder cancer cells[5]. MMP-1 was significantly decreased in ESCC cells treated with cabozantinib, which was the reason for the decreased migration activity of ESCC cells treated with cabozantinib[6]. Cabozantinib inhibits tumor growth in a dose-dependent manner in human tumor models in rodents[1]. In vivo pharmacodynamic studies showed substantial inhibition of RET in TT xenograft tumors following a single oral dose of cabozantinib[7]. Cabozantinib showed excellent antitumor effects in vivo using CRC(colorectal cancer) explants model[8]. References: |