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    DCC-2618
    DCC-2618

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V3284
    CAS #: 1442472-39-0; DCC-2618 HClPurity ≥98%

    Description: DCC-2618 (Ripretinib) is a potent, orally bioactive, and spectrum-selective pan KIT and PDGFRA inhibitor which blocks KIT D816V and multiple other kinase targets relevant to systemic mastocytosis. DCC-2618 inhibits the proliferation and survival of various human mast cell lines (e.g. HMC-1, ROSA, MCPV-1) as well as primary neoplastic mast cells obtained from patients with advanced systemic mastocytosis (IC50<1 μM). Moreover, DCC-2618 decreased growth and survival of primary neoplastic eosinophils obtained from patients with systemic mastocytosis or eosinophilic leukemia, leukemic monocytes obtained from patients with chronic myelomonocytic leukemia with or without concomitant systemic mastocytosis, and blast cells obtained from patients with acute myeloid leukemia. DCC-2618 is effective in vivo in patients with advanced systemic mastocytosis and is currently under investigation in clinical trials. 

    References:  2018 May;103(5):799-809;  2017 Feb;7(2):121-122. 


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    Molecular Weight (MW) 510.37
    FormulaC24H21BrFN5O2
    CAS No.1442472-39-0; 1225278-16-9 (wrong)    
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: >100 mg/mL 
    Water: <1 mg/mL 
    Ethanol:  10 mg/mL 
    Chemical Name1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3-phenylurea
    SynonymsDCC-2618; DCC 2618; DCC2618; Ripretinib
    SMILES CodeO=C(NC1=CC(C2=CC3=C(C=C(NC)N=C3)N(CC)C2=O)=C(Br)C=C1F)NC4=CC=CC=C4


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    In Vitro

    In vitro activity: DCC-2618 is a potent, orally bioactive, and spectrum-selective pan KIT and PDGFRA inhibitor which blocks KIT D816V and multiple other kinase targets relevant to systemic mastocytosis. DCC-2618 inhibits the proliferation and survival of various human mast cell lines (e.g. HMC-1, ROSA, MCPV-1) as well as primary neoplastic mast cells obtained from patients with advanced systemic mastocytosis (IC50<1 μM). Moreover, DCC-2618 decreased growth and survival of primary neoplastic eosinophils obtained from patients with systemic mastocytosis or eosinophilic leukemia, leukemic monocytes obtained from patients with chronic myelomonocytic leukemia with or without concomitant systemic mastocytosis, and blast cells obtained from patients with acute myeloid leukemia. DCC-2618 is effective in vivo in patients with advanced systemic mastocytosis and is currently under investigation in clinical trials. 


    Kinase Assay: For evaluation of KIT and BTK signaling, HMC-1.1, HMC-1.2, ROSAKIT WT and ROSAKIT D816V cells were incubated in control medium or in DCC-2618 (0.5–5 μM) for 4 h at 37°C. Western blotting was performed essentially as described elsewhere. For evaluation of downstream signaling pathways of KIT, HMC-1.1, HMC-1.2, ROSAKIT WT and ROSAKIT D816V cells were first pre- incubated overnight in Iscove modified Dulbecco medium devoid of fetal calf serum and of stem cell factor. Cells (106) from each line were then treated with DCC-2618 (0.001–10 μM) for 90 min at 37°C. At the end of the treatment, ROSAKIT WT cells were stimulated with stem cell factor-containing supernatants (10%) of Chinese hamster ovary cells transfected with the murine scf (kl) gene (CHO-KL) at room temperature for 10 min. Thereafter, Western blotting was performed essentially as described previously.


    Cell Assay: Drug-exposed cells (cell lines or primary cells) were analyzed for proliferation and survival. The bioassays employed are described in the Online Supplementary Methods

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    References  2018 May;103(5):799-809.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    DCC-2618

    DCC-2618 and its active metabolite DP-5439 inhibit proliferation of neoplastic mast cells.  2018 May;103(5):799-809.

    DCC-2618

    DCC-2618 inhibits phosphorylation of KIT and other targets in neoplastic mast cells.  2018 May;103(5):799-809.

    DCC-2618

    Effects of DCC-2618 on anti-IgE-induced histamine release from normal basophils.  2018 May;103(5):799-809.

    DCC-2618

    DCC-2618 and DP-5439 induce apoptosis in neoplastic mast cells.  2018 May;103(5):799-809.

    DCC-2618

    Effects of DCC-2618 and DP-5439 on proliferation and survival of acute myeloid leukemia (AML) and chronic myelomonocytic leukemia (CMML).  2018 May;103(5):799-809.



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