Norcantharidin

Catalog No.S3759 Synonyms: Endothall anhydride

For research use only.

Norcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.

Norcantharidin Chemical Structure

CAS No. 29745-04-8

Purity & Quality Control

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Biological Activity

Description Norcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.
Targets
c-Met [1]
()
EGFR [1]
()
In vitro

Norcantharidin (NCTD) induces cell cycle arrest at G2/M phase in HCT116 and HT29 cells. NCTD suppresses not only the expression of the total EGFR and the phosphorylated EGFR but also the expression of the total c-Met and the phosphorylated c-Met in colon cancer cells[1]. Norcantharidin (NCTD) is an inhibitor of protein phosphatase types 1, 2A and 2B, arrests the cell cycle at G2/M phase in K562 human myeloid leukemia cells, and inhibits DNA synthesis in HL-60 cells[2].

In vivo Norcantharidin (NCTD) inhibits the growth of the xenografted tumors in a dose- and time-dependent manner. Tumor volume decreases with an increased tumor inhibitory rate in the NTCD group compared with the control group. The apoptosis rate increases along with a decreased percentage of cells in S phase in the NTCD group compared with the control group. The morphological changes of apoptosis such as nuclear shrinkage, chromatin aggregation, chromosome condensation, and typical apoptosis bodies in the xenografted tumor cells induced by NCTD are observed. The expression of cyclin-D1, Bcl-2 and survivin proteins/mRNAs decrease significantly, with increased expression of p27 and Bax proteins/mRNAs in the NCTD group compared with the control group. NCTD is reported clinically as an anti-tumor drug against hepatoma, esophageal and gastric carcinoma, and leucopenia[2].

Protocol (from reference)

Cell Research:[1]
  • Cell lines: HT29 and HCT116 cells
  • Concentrations: 6.25 to 100 μM
  • Incubation Time: 24, 48, or 72 h
  • Method: HT29 and HCT116 cells suspended in complete media are seeded in 96-well plates (2000 cells/well). After growing for 24 h in incubator, media are aspirated and 0.2 mL complete media containing serial concentrations of NCTD are added to each well. After incubating the plate for 24, 48, or 72 h, 20 μL of resazurin (2 mg/mL dissolved in water) is added to each well. The fluorescent signal is monitored using 544 nm excitation and 595 nm emission wavelengths by Spectramax M5 plate reader after incubation at 37 °C for 16 h in the incubator. The number of living cells in each well is proportional to the relative fluorescence unit (RFU) measured by the assay.
Animal Research:[2]
  • Animal Models: The tumor xenograft model of human gallbladder carcinoma in nude mice
  • Dosages: 24 mg/kg and 28 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

DMSO 33 mg/mL
(196.25 mM)


Chemical Information

Molecular Weight 168.15
Formula

C8H8O4

CAS No. 29745-04-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC2C3C(C1O2)C(=O)OC3=O

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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