IKP-104 is a microtubule/tubulin inhibitor (IC50 = 1.31 μM) that halts cells in mitosis and the M phase by inhibiting microtubule assembly and inducing cytoskeleton microtubule depolymerization. It suppresses the growth of both murine and human tumor cell lines, exhibiting antitumor effects in mouse ascites tumor and lung cancer models. IKP-104 is applicable in research on cancers such as leukemia, lung cancer, and melanoma.

IKP-104 (0-25 μM) inhibits the aggregation of tau-induced ungraded tubulin and homotypic pure αβII and αβIV, without affecting αβIII. A concentration of IKP-104 (1.5 μM) encourages aggregation of preformed microtubules (ungraded tubulin and αβIII) and helices (homotypic αβII), while not altering the morphology of microtubules formed by αβIV. Additionally, KP-104 (0-40 μM, 0-40 minutes) leads to increased absorbance, modifies aggregate formation, and changes the morphology of existing microtubules. KP-104 exhibits cytotoxicity towards L1210, B16, Lewis, K562, and HeLa cells with IC50 values of 0.0025, 5.2, 0.0017, 0.0012, and 0.015 μg/mL, respectively. At a concentration of 3.6 μg/mL over 0-48 hours, KP-104 increases the proportion of spherical cells by inhibiting microtubule polymerization and inducing their depolymerization in B16 cells, arresting them at the M phase and mitotic phase.

IKP-104, administered at doses of 0.5-5 mg/kg either intraperitoneally or subcutaneously once daily for 5-9 days, demonstrates antitumor activity in mouse models of ascites tumors and Lewis lung carcinoma.