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Description: DCC-2618 (Ripretinib) is a potent, orally bioactive, and spectrum-selective pan KIT and PDGFRA inhibitor which blocks KIT D816V and multiple other kinase targets relevant to systemic mastocytosis. DCC-2618 inhibits the proliferation and survival of various human mast cell lines (e.g. HMC-1, ROSA, MCPV-1) as well as primary neoplastic mast cells obtained from patients with advanced systemic mastocytosis (IC50< 1 uM). Moreover, DCC-2618 decreased growth and survival of primary neoplastic eosinophils obtained from patients with systemic mastocytosis or eosinophilic leukemia, leukemic monocytes obtained from patients with chronic myelomonocytic leukemia with or without concomitant systemic mastocytosis, and blast cells obtained from patients with acute myeloid leukemia. DCC-2618 is effective in vivo in patients with advanced systemic mastocytosis and is currently under investigation in clinical trials.
References: Haematologica. 2018 May; 103(5):799-809; Cancer Discov. 2017 Feb; 7(2):121-122.
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