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
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Biological Information

  • Product Name
    DCC-2618
  • Note
    Research use only, not for human use.
  • Brief Description
    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).
  • Description
    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), 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.
  • 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.
  • In Vivo
    ——
  • Synonyms
    Ripretinib | DCC2618
  • Pathway
    Angiogenesis
  • Target
    c-Kit
  • Recptor
    c-Kit
  • Research Area
    Cancer
  • Indication
    Gastric Cancer

Chemical Information

  • CAS Number
    1442472-39-0
  • Formula Weight
    510.367
  • Molecular Formula
    C24H21BrFN5O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : 45 mg/mL 88.17 mM
  • SMILES
    CCN1C2=CC(=NC=C2C=C(C1=O)C3=CC(=C(C=C3Br)F)NC(=O)NC4=CC=CC=C4)NC
  • Chemical Name
    1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3-phenylurea

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • 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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