Ripretinib (DCC-2618)|CAS 1442472-39-0|DC Chemicals

Cas No.:	1442472-39-0
Chemical Name:	Ripretinib free base
Synonyms:	DCC-2618; DCC 2618; DCC2618; Ripretinib;
SMILES:	CCN1C2=CC(=NC=C2C=C(C1=O)C3=CC(=C(C=C3Br)F)NC(=O)NC4=CC=CC=C4)NC
Formula:	C₂₄H₂₁BrFN₅O₂
M.Wt:	510.37
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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

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