1442472-39-0

1442472-39-0 structure

Name: DCC-2618
Chemical Name: DCC-2618
CAS Number: 1442472-39-0
Molecular Formula: C₂₄H₂₁BrFN₅O₂
Molecular Weight: 510.36
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK c-Kit
Create Date: 2018-02-10 19:16:00
Modify Date: 2024-01-03 08:12:36
Ripretinib (DCC-2618) is a pan-KIT and PDGFRA inhibitor, and has antitumor activity.

Name	DCC-2618

Description	Ripretinib (DCC-2618) is a pan-KIT and PDGFRA inhibitor, and has antitumor activity.
Related Catalog	Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit Research Areas >> Cancer
Target	PDGFRA KIT
In Vitro	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].
References	[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.