2. Protein Tyrosine Kinase/RTK
  3. c-Kit PDGFR
  4. Avapritinib

Avapritinib (BLU-285) est un inhibiteur de KIT et de PDGFRA des kinases mutantes de la boucle d'activation qui est très puissant, sélectif et oralement actif avec IC50s de 0,27 et de 0,24 nM pour les KIT D816V et PDGFRA D842V, respectivement. Avapritinib (BLU-285) se lie à la conformation active de la kinase et présente une activité antitumorale. Avapritinib (BLU-285) atténue la fonction de transport des deux ABCB1 et ABCG2.

Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2.

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

CAS No. : 1703793-34-3

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ready for reconstitution
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Based on 12 publication(s) in Google Scholar

Other Forms of Avapritinib:

Avapritinib Related Antibodies

Top Publications Citing Use of Products

    Avapritinib purchased from MedChemExpress. Usage Cited in: Neuron. 2025 Aug 27:S0896-6273(25)00591-4.  [Abstract]

    Avapritinib treatment (50 mg/kg/day) was administered. Representative immunohistochemistry images of Ki67+ cells were shown.

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

    PDGFRA D842V phosphorylation and total PDGFRA were assessed following a 2-hour treatment with DMSO (vehicle) or 1, 10, 100 nM concentrations of Avapritinib.

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

    PDGFRA was treated with Avapritinib, crenolanib, dasatinib, lenvatinib, or ripretinib for 72 h.

    Avapritinib purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Feb 25;26(5):1980.

    The cytotoxicity of BLU-258 alone and in aggregates with Congo red (CR-BLU-258) on pancreatic cell lines was assessed using an LDH assay after 48 h of incubation.

    Avapritinib purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Feb 25;26(5):1980.

    The morphology of the 3D cell cultures of BxPC3 cells was incubated for 48 h with BLU-258 or CR-BLU-258 and without the tested compounds; scale bar = 200 μm.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2[1][2].

    IC50 & Target

    IC50: 0.27 nM (KIT D816V), 0.24 nM (PDGFRA D842V)[1]
    Cellular Effect
    Cell Line Type Value Description References
    BaF3 GI50
    4.075 μM
    Compound: 5; BLU-285
    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

    Avapritinib (BLU-285) has demonstrated biochemical in vitro activity on the KIT exon 17 mutant enzyme, KIT D816V (IC50=0.27 nM). Cellular activity of Avapritinib on KIT D816 mutants is measured by autophosphorylation in the human mast cell leukemia cell line HMC1.2, and the P815 mouse mastocytoma cell line with IC50=4 and 22 nM, respectively. In Kasumi-1 cells, a t(8;21)-positive AML cell line with a KIT exon 17 N822K mutation, Avapritinib potently inhibits KIT N822K mutant autophosphorylation (IC50=40 nM), downstream signaling, as well as cellular proliferation (IC50=75 nM)[3].

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

    Avapritinib Related Antibodies
    In Vivo

    In vivo Avapritinib (BLU-285) is well tolerated and has demonstrated dose dependent antitumor efficacy. Complete tumor growth inhibition and ≥75% KIT kinase inhibition is observed with 10 mg/kg once daily, oral dosing of Avapritinib in the aggressive KIT exon 17 mutant driven P815 mastocytoma model grown as a solid tumor allograft as well as in a disseminated model of disease. Disease burden, measured by whole body luciferase imaging (photons/second/mm2), increases 86-fold in the vehicle control animals over the 24 day dosing period with widespread disease detectable in both femurs, the pelvis and circulating in peripheral blood. Avapritinib at both doses (10 or 30 mg/kg orally, once daily) results in a marked reduction of disease burden throughout the study. Avapritinib at either 10 or 30 mg/kg results in tumor regression in all animals with disease abrogation indistinguishable from background signal measurements in several animals by the end of study. Avapritinib is also well tolerated in this in vivo model and has no adverse effects on body weight at either dose[3].

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

    498.56

    Formula

    C26H27FN10
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    CN1N=CC(C2=CN3C(C(N4CCN(C5=NC=C([C@@](C)(N)C6=CC=C(F)C=C6)C=N5)CC4)=NC=N3)=C2)=C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 83.33 mg/mL (167.14 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0058 mL 10.0289 mL 20.0578 mL
    5 mM 0.4012 mL 2.0058 mL 4.0116 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    V2

    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: ≥ 2.5 mg/mL (5.01 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.01 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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

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    (per animal)

    g

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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 +
    % 
    +
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    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: 99.85%

    SDS (393 KB)

    COA (252 KB) HNMR (140 KB) RP-HPLC (245 KB) MS (68 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [1]

    Mice[1]
    A Kasumi-1 luc+ AML NOG SCID mouse femoral injection model is used to assess the efficacy of Avapritinib (BLU-285) in KIT exon 17-mutated CBF-AML. Following a 21 day post injection latency period, mice are dosed with Avapritinib orally, once daily at 10 mg/kg or 30 mg/kg through day 45.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0058 mL 10.0289 mL 20.0578 mL 50.1444 mL
    5 mM 0.4012 mL 2.0058 mL 4.0116 mL 10.0289 mL
    10 mM 0.2006 mL 1.0029 mL 2.0058 mL 5.0144 mL
    15 mM 0.1337 mL 0.6686 mL 1.3372 mL 3.3430 mL
    20 mM 0.1003 mL 0.5014 mL 1.0029 mL 2.5072 mL
    25 mM 0.0802 mL 0.4012 mL 0.8023 mL 2.0058 mL
    30 mM 0.0669 mL 0.3343 mL 0.6686 mL 1.6715 mL
    40 mM 0.0501 mL 0.2507 mL 0.5014 mL 1.2536 mL
    50 mM 0.0401 mL 0.2006 mL 0.4012 mL 1.0029 mL
    60 mM 0.0334 mL 0.1671 mL 0.3343 mL 0.8357 mL
    80 mM 0.0251 mL 0.1254 mL 0.2507 mL 0.6268 mL
    100 mM 0.0201 mL 0.1003 mL 0.2006 mL 0.5014 mL
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    Avapritinib 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:

    Avapritinib1703793-34-3BLU-285BLU285BLU 285c-KitPDGFRSCFRCD117Platelet-derived growth factor receptorInhibitorinhibitorinhibit

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