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Norcantharidin EGFR inhibitor

Cat.No.S3759

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

Chemical Structure

Molecular Weight: 168.15

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Quality Control

Batch: S375901 DMSO]33 mg/mL]false]]]false]]]false Purity: 98%
98

Chemical Information, Storage & Stability

Molecular Weight 168.15 Formula

C8H8O4

 Storage (From the date of receipt)
CAS No. 29745-04-8 Download SDF Storage of Stock Solutions

Synonyms Endothall anhydride Smiles C1CC2C3C(C1O2)C(=O)OC3=O

Solubility

In vitro
Batch:

DMSO : 33 mg/mL (196.25 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

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Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
c-Met [1]
EGFR [1]
In vitro
Norcantharidin (NCTD) induces cell cycle arrest at G2/M phase in HCT116 and HT29 cells. This compound 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]. It 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 this compound 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. This chemical is reported clinically as an anti-tumor drug against hepatoma, esophageal and gastric carcinoma, and leucopenia[2].
References

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