Mipsagargin

CAS NO.: 1245732-48-2
Molecular Formula: C66H100N6O27
Molecular Weight: 1409.52
Appearance: White Powder
Purity: ≥98.0%
Solubility: Generally soluble in water, DMSO, and other organic solvents

Function
Mipsagargin exerts its effects primarily by specifically binding to integrin αvβ3, which is overexpressed on the surface of tumor cells. Integrin αvβ3 plays a pivotal role in processes such as tumor angiogenesis, tumor cell migration, and invasion. Upon binding to integrin αvβ3, Mipsagargin disrupts the interaction between tumor cells and the extracellular matrix, thereby inhibiting tumor angiogenesis and metastasis. Furthermore, it may induce apoptosis in tumor cells by activating intracellular apoptotic signaling pathways.
Currently, research into Mipsagargin for cancer therapy is attracting significant attention. Preclinical studies have demonstrated promising anti-tumor activity across various tumor models, including melanoma, breast cancer, and colorectal cancer.

Description About Mipsagargin
Mipsagargin is a novel prodrug targeting tumor vasculature; it achieves precise release of its active component through enzymatic activation, thereby significantly reducing side effects and representing a breakthrough in cancer therapy. Based on the structure of thapsigargin, it features a complex chemical architecture comprising structural units such as polycyclic rings, esters, and peptide chains. It is designed to release its active ingredient at specific targets within the body, enabling targeted drug delivery. By leveraging a targeted delivery system, it can be selectively activated to release its active pharmaceutical component within the tumor microenvironment.
Mipsagargin has undergone preclinical and early-stage clinical studies in various PSMA-positive tumors—including hepatocellular carcinoma, prostate cancer, and renal cancer—demonstrating favorable pharmacokinetic properties and preliminary efficacy. In liver cancer models, Mipsagargin selectively induces tumor necrosis while remaining largely inactive in normal liver tissue, thereby minimizing toxic side effects.