ONT-093

ONT-093 (OC 144-093) is a potent and orally active inhibitor of P-glycoprotein pump. ONT-093 inhibits P-gp-mediated ATPase activity with an IC₅₀ of 0.16 μM. ONT-093 can inhibit drug efflux and increase bioavailability. ONT-093 reverses cancer cells multidrug resistance to chemotherapeutic drugs. ONT-093 can be used for the researches of cancer and infection, such as colon cancer and malarial ^[1][2][3]. In Vitro:ONT-093 reverses multidrug resistance (MDR) to Doxorubicin (HY-15142A), Paclitaxel (HY-B0015), and Vinblastine in lymphoma, breast, ovarian, uterine, and colorectal carcinoma cell lines expressing P-glycoprotein with an average EC₅₀ of 0.032 μM^[1].
ONT-093 shows no cytotoxic against 15 normal, nontransformed, or tumor cell lines, with an average cytostatic IC₅₀ of >60 μM^[1].
ONT-093 (10 μM) reverses the diminished Halofantrine (HY-A0148) accumulation by pfmdr1^Dd2- expressingoocytes^[3].
In Vivo:ONT-093 (5-20 mg/kg, i.p., at days 0, 1, 4, 5, 8, and 9) increases the life span of Doxorubicin (HY-15142A)-treated m in mice engrafted with MDR P388 leukemia cells^[1].
ONT-093 (30 mg/kg, i.g., twice a day at days 4-6, 11-13, 18-20 and 25-27) enhances the antitumor activity of Paclitaxel (HY-B0015) in MDR breast and colon carcinoma xenograft mice models^[1].