E7130 is a microtubule inhibitor that enhances the tumor microenvironment by inhibiting cancer-associated fibroblasts and facilitating the remodeling of the tumor vasculature system.

E7130 disrupts microtubule dynamics and demonstrates antiproliferative activity in cancer cell lines KPL-4, OSC-19, FaDu, and HSC-2, with IC50 values ranging from 0.01-0.1 nM. At a concentration of 0.15 nM, E7130 inhibits TGF-β-induced myofibroblast transformation by disrupting microtubule network formation and inactivating the PI3K/AKT/mTOR pathway.

Administered intravenously at doses of 45-180 μg/kg, E7130 increases microvascular density (MVD) within tumors, enhancing the delivery of cetuximab (CTX) and leading to tumor regression in HSC-2 SCCHN xenograft BALB/c mice. Additionally, E7130 reduces α-SMA-positive cancer-associated fibroblasts (CAF), and the combination of E7130 and CTX modifies fibroblast phenotypes in FaDu SCCHN xenograft BALB/c mice.