Oxamflatin (Metacept-3) is a selective histone deacetylase (HDAC) inhibitor characterized by high potency (IC50 = 15.7 nM) and the presence of an alkyne group capable of undergoing azide-alkyne cycloaddition reactions (CuAAc).

HDAC:15.7 nM

Methods: HeLa cells were cultured for 24 hours, and 1 mg/ml of Oxamflatin (Metacept-3) was added to the cultures at 0 hours. After the indicated incubation times, cells were harvested and their isolated nuclei were analyzed by flow cytometry; the distribution of cells in the cell cycle was determined using ModFit LT software.
Results: Oxamflatin caused HeLa cells to have an elongated cell shape with filamentous processes and cell cycle arrest in the G1 phase. [1]

Methods: Oxamflatin (Metacept-3) (8±50 mg/kg, intraperitoneal injection) was used in mice with B16 melanoma cell tumor xenografts at days 1, 3, 5, 7, 9, and 11 after inoculation. The increase in lifespan (ILS) of mice transplanted with B16 murine melanoma tumors after treatment with oxam¯atin was measured, and the number of days of survival was calculated and the ILS% was calculated.
Results: Six injections of oxamflatin at a dose of 20 mg/kg each time significantly increased the number of days of survival of mice (38% of ILS); the ILS of mice treated with 50 mg/kg of oxamflatin was calculated to be over 67%, and one mouse survived for more than 60 days after tumor inoculation. No side effects such as weight loss were observed, at least until this dose. [1]