2. Protein Tyrosine Kinase/RTK Apoptosis
  3. c-Kit PDGFR FLT3 VEGFR Apoptosis
  4. Ripretinib

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). DCC-2618 exerts antineoplastic effect and induces apoptosis.

For research use only. We do not sell to patients.

CAS No. : 1442472-39-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Ripretinib:

Ripretinib Related Antibodies

Top Publications Citing Use of Products

    Ripretinib purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Jul;21(7):1523-1543.  [Abstract]

    Ripretinib (10-2-102 μM; 24 h) induced apoptosis of WaGa cells.

    Ripretinib purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Jul;21(7):1523-1543.  [Abstract]

    Ripretinib (0.1-20 μM; 24 h) reduced KIT phosphorylation and increased cleaved PARP levels in WaGa cells.

    Ripretinib purchased from MedChemExpress. Usage Cited in: NPJ Precis Oncol. 2025 Aug 16;9(1):289.  [Abstract]

    Ripretinib (1-100 nM; 2 h) significantly inhibited PDGFRA autophosphorylation in Ba/F3 cells expressing MDM2::PDGFRA or PDGFRA D842V.

    Ripretinib purchased from MedChemExpress. Usage Cited in: NPJ Precis Oncol. 2025 Aug 16;9(1):289.  [Abstract]

    Dose-response cell viability of onco-addicted Ba/F3 cells expressing MDM2::PDGFRA after treatment with Ripretinib (0.0001-10000 nM; 72 h).

    Ripretinib purchased from MedChemExpress. Usage Cited in: Clin Genitourin Cancer. 2025 Aug;23(4):102359.

    Ripretinib (1 μM; 120 h) decreased viability of three ChRCC cell lines (RCJ-T1, RCJ-T2, and RCJ-M).

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    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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].

    IC50 & Target[1][2]

    PDGFRA

     

    KIT

     

    Cellular Effect
    Cell Line Type Value Description References
    BaF3 GI50
    8.037 μM
    Compound: 4; DCC-2618
    Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay
    Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay
    		[PMID: 30204441]
    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[2].
    Ripretinib (DCC-2618) is a pan-KIT and PDGFRA inhibitor, shows cytotoxic activity against gastrointestinal stromal tumors[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Ripretinib Related Antibodies
    Clinical Trial
    Molecular Weight

    510.36

    Formula

    C24H21BrFN5O2
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(NC1=CC(C2=CC3=C(C=C(NC)N=C3)N(CC)C2=O)=C(Br)C=C1F)NC4=CC=CC=C4
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (48.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9594 mL 9.7970 mL 19.5940 mL
    5 mM 0.3919 mL 1.9594 mL 3.9188 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.08 mg/mL (4.08 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (4.08 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 98.90%

    SDS (393 KB)

    COA (248 KB) HNMR (211 KB) LCMS (111 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9594 mL 9.7970 mL 19.5940 mL 48.9850 mL
    5 mM 0.3919 mL 1.9594 mL 3.9188 mL 9.7970 mL
    10 mM 0.1959 mL 0.9797 mL 1.9594 mL 4.8985 mL
    15 mM 0.1306 mL 0.6531 mL 1.3063 mL 3.2657 mL
    20 mM 0.0980 mL 0.4899 mL 0.9797 mL 2.4493 mL
    25 mM 0.0784 mL 0.3919 mL 0.7838 mL 1.9594 mL
    30 mM 0.0653 mL 0.3266 mL 0.6531 mL 1.6328 mL
    40 mM 0.0490 mL 0.2449 mL 0.4899 mL 1.2246 mL
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    Ripretinib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Ripretinib1442472-39-0DCC-2618DCC2618DCC 2618c-KitPDGFRFLT3VEGFRApoptosisSCFRCD117Platelet-derived growth factor receptorCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Vascular endothelial growth factor receptorInhibitorinhibitorinhibit

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