Norcantharidin

Catalog No.S3759 Batch:S375901

Technical Data

Formula	C₈H₈O₄
Molecular Weight	168.15	CAS No.	29745-04-8
Solubility (25°C)*	In vitro	DMSO	33 mg/mL (196.25 mM)


* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 Assay:^{^[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 Study:^{^[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.

Cell Assay:^{^[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 Study:^{^[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.

References

Selleck's Norcantharidin has been cited by 2 publications

Antitumor effect of luteolin proven by patient-derived organoids of gastric cancer [ Phytother Res, 2023, 10.1002/ptr.7963]	PubMed: 37469042
Norcantharidin ameliorates estrogen deficient-mediated bone loss by attenuating the activation of extracellular signal-regulated kinase/ROS/NLRP3 inflammasome signaling [ Front Pharmacol, 2022, 13:1019478]	PubMed: 36408264

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SHIPPING AND STORAGE
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