| Description | (±)-Norcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers. |
| In vivo | NCTD might be a useful and inexpensive drug candidate to substitute for gefitinib to serve the treatment needs of cancer patients[1].NCTD inhibits the growth of xenografted tumors of human gallbladder carcinoma in nude mice by inducing apoptosis and blocking the cell cycle in vivo[2]. |
| Cell experiments | Two human colon cancer cell lines, HCT116 and HT29, were used as model systems to investigate the anti-cancer molecular mechanism of NCTD. Cell cycle arrest and early/late apoptosis were analyzed by flow cytometry. The levels of EGFR, phospho-EGFR, c-Met, phospho-c-Met and other related proteins were quantified by western blot analysis[1] |
| Animal experiments | The tumor xenograft model of human gallbladder carcinoma in nude mice in vivo was established with subcutaneous GBC-SD cells. The experimental mice were randomly divided into control, 5-FU, NCTD, and NCTD+5-FU groups which were given different treatments. Tumor growth in terms of size, growth curve, and inhibitory rate was evaluated. Cell cycle, apoptosis, and morphological changes of the xenografted tumors were assessed by flow cytometry and light/electron microscopy. The expression of the cell cycle-related proteins cyclin-D1 and p27 as well as the apoptosis-related proteins Bcl-2, Bax, and survivin were determined by the streptavidin-biotin complex (SABC) method and RT-PCR[2]. |
| Synonyms | Endothall anhydride, 去甲斑蝥素, Norcantharidin |
| molecular weight | 168.15 |
| Molecular formula | C8H8O4 |
| CAS | 29745-04-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 33 mg/mL (196.25 mM) |
| References | 1. Qiu P , Wang S , Liu M , et al. Norcantharidin Inhibits cell growth by suppressing the expression and phosphorylation of both EGFR and c-Met in human colon cancer cells[J]. BMC Cancer, 2017, 17(1):55. 2. Fan Y Z , Zhao Z M , Fu J Y , et al. Norcantharidin Inhibits Growth of Human Gallbladder Carcinoma Xenografted Tumors in Nude Mice by Inducing Apoptosis and Blocking the Cell Cycle in vivo[J]. Hepatobiliary & Pancreatic Diseases International, 2010, 9(4):414-422. |