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Compound 8c (Shanghai Institute of Materia Medica)

Development stage
Preclinical
Lead developer
Shanghai Institute of Materia Medica
Modality
Small Molecules
Administration
Intravenous
01

Overview

Compound 8c (PI3K/AKT-IN-3) is a synthetic triterpene-nucleoside conjugate developed by the Shanghai Institute of Materia Medica, Chinese Academy of Sciences. It was created by conjugating methylated betulonic acid with the nucleoside derivative azidothymidine (AZT) to enhance the water solubility and antitumor potency of the parent pentacyclic triterpene. The compound exhibits broad-spectrum antitumor activity by inhibiting the PI3K/Akt/mTOR signaling pathway, which subsequently induces both autophagy and apoptosis in cancer cells. Preclinical studies have demonstrated significant efficacy against hepatocellular carcinoma, esophageal squamous cell carcinoma, and colorectal cancer cell lines. In xenograft mouse models of hepatocellular carcinoma, Compound 8c showed tumor growth inhibition comparable to the standard chemotherapy agent paclitaxel.

Other names
methylated betulonic acid-azidothymidine conjugatemethylated betulonic acid-azidothymidine compound
02

Targets

THRB (Thyroid hormone receptor beta)

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