DCC-2618
CAS No. 1442472-39-0
DCC-2618( Ripretinib | DCC2618 )
Catalog No. M11875 CAS No. 1442472-39-0
DCC-2618 (Ripretinib, DCC2618) is a potent, oral inhibitor of singly and doubly mutated KIT with IC50 of WT (IC50=4 nM), V654A (8 nM), T670I (18 nM), D816H (5 nM).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
Size | Price / USD | Stock | Quantity |
2MG | 88 | In Stock |
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5MG | 151 | In Stock |
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10MG | 260 | In Stock |
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25MG | 443 | In Stock |
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50MG | 645 | In Stock |
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100MG | 888 | In Stock |
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500MG | 1782 | In Stock |
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1G | Get Quote | In Stock |
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Biological Information
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Product NameDCC-2618
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NoteResearch use only, not for human use.
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Brief DescriptionDCC-2618 (Ripretinib, DCC2618) is a potent, oral inhibitor of singly and doubly mutated KIT with IC50 of WT (IC50=4 nM), V654A (8 nM), T670I (18 nM), D816H (5 nM).
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DescriptionDCC-2618 (Ripretinib, DCC2618) is a potent, oral inhibitor of singly and doubly mutated KIT with IC50 of WT (IC50=4 nM), V654A (8 nM), T670I (18 nM), D816H (5 nM), D816V; also inhibits PDGFRα/β, KDR and cFMS, robustly inhibits exon 17, exon 9/13, exon 9/14, and exon 9/17 KIT mutants, as well as exon 11/17 KIT mutants; inhibits wild type and mutant KIT phosphorylation in cancer cells, demonstrates the potential to treat KIT mutant-driven cancers including GIST, systemic mastocytosis, AML, or melanoma.Gastric Cancer Phase 3 Clinical(In Vitro):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.Ripretinib (DCC-2618) is a pan-KIT and PDGFRA inhibitor, shows cytotoxic activity against gastrointestinal stromal tumors.
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In VitroRipretinib (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.Ripretinib (DCC-2618) is a pan-KIT and PDGFRA inhibitor, shows cytotoxic activity against gastrointestinal stromal tumors.
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In Vivo——
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SynonymsRipretinib | DCC2618
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PathwayAngiogenesis
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Targetc-Kit
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Recptorc-Kit
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Research AreaCancer
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IndicationGastric Cancer
Chemical Information
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CAS Number1442472-39-0
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Formula Weight510.367
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Molecular FormulaC24H21BrFN5O2
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Purity>98% (HPLC)
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SolubilityDMSO : 45 mg/mL 88.17 mM
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SMILESCCN1C2=CC(=NC=C2C=C(C1=O)C3=CC(=C(C=C3Br)F)NC(=O)NC4=CC=CC=C4)NC
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Chemical Name1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3-phenylurea
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Mathias A Schneeweiss, et al. Blood 2016 128:1965.
2. Cancer Discov. 2017 Feb;7(2):121-122. doi: 10.1158/2159-8290.
molnova catalog
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