Ripretinib (Synonyms: DCC-2618) |
| Catalog No.GC37538 |
Le riprétinib (DCC-2618) est un inhibiteur de contrÔle de commutation KIT et PDGFRA biodisponible par voie orale. Le riprétinib (DCC-2618) cible et se lie À la fois aux formes de type sauvage et mutantes de KIT et de PDGFRA spécifiquement au niveau de leurs sites de liaison de poche de commutation, empêchant ainsi le passage de conformations inactives À actives de ces kinases et inactivant leurs formes de type sauvage et mutantes . Le riprétinib (DCC-2618) inhibe également plusieurs autres cibles kinases, telles que FLT3 et KDR (ou VEGFR-2). Le DCC-2618 exerce un effet antinéoplasique et induit l'apoptose.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1442472-39-0
Sample solution is provided at 25 µL, 10mM.
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Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2)[1][2]. DCC-2618 exerts antineoplastic effect and induces apoptosis[3].
Ripretinib (DCC-2618) 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].Ripretinib (DCC-2618) is a pan-KIT and PDGFRA inhibitor, shows cytotoxic activity against gastrointestinal stromal tumors[4].
References:
[1]. 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.
[2]. KIT/PDGFR Inhibitor DCC-2618.
[3]. 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.
[4]. BLU-285, DCC-2618 Show Activity against GIST. Cancer Discov. 2017 Feb;7(2):121-122.
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