DCC-2618

Ripretinib (DCC-2618) is a pan-KIT and PDGFRA inhibitor, and has antitumor activity.

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit

Research Areas >> Cancer

PDGFRA

KIT

Ripretinib is a pan-KIT and PDGFRA inhibitor, shows cytotoxic activity against gastrointestinal stromal tumors[1]. Ripretinib suppresses phosphorylation of KIT and decreases the expression of phosphosphorylated (p)STAT5, pAKT and pERK1/2 in neoplastic mast cells. Ripretinib inhibits the growth of ROSAKIT K509I cells with an IC50 of 34 ± 10 nM, and also induces apoptosis in these cells. Ripretinib (0.1-1.0 μM) inhibits IgE-dependent histamine release from basophils and spontaneous tryptase release from neoplastic mast cells, and also counteracts growth and survival of leukemic monocytes and blast cells at 0.01-5 μM[2].

[1]. BLU-285, DCC-2618 Show Activity against GIST. Cancer Discov. 2017 Feb;7(2):121-122.

[2]. Schneeweiss M, et al. The KIT and PDGFRA switch-control inhibitor DCC-2618 blocks growth and survival of multiple neoplastic cell types in advanced mastocytosis. Haematologica. 2018 May;103(5):799-809.

Pexidartinib | Nintedanib (BIBF 1120) | Crenolanib | SU 5402 | Linifanib (ABT-869) | Cediranib | Masitinib (AB1010) | SU14813 | Dovitinib (TKI-258, CHIR-258) | Sitravatinib (MGCD516) | CHIR-124 | CP-673451 | DCC-2618 | BLU-285 | Motesanib