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

Avapritinib  (Synonyms: BLU-285)

製品番号: HY-101561 純度: 99.75%
COA 取扱説明書 Technical Support

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 1703793-34-3

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 99 在庫あり
Solution
10 mM * 1 mL in DMSO USD 99 在庫あり
Solid
5 mg $90 在庫あり
10 mg $150 在庫あり
25 mg $300 在庫あり
50 mg $450 在庫あり
100 mg $750 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 12 publication(s) in Google Scholar

Other Forms of Avapritinib:

Avapritinib 関連抗体

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.

    PDGFR アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    PDGFR PDGFRβ PDGFRα

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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]
    体外実験

    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 関連抗体
    体内実験

    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.
    臨床実験
    分子量

    498.56

    分子式

    C26H27FN10
    CAS 番号
    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
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    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
    10 mM 0.2006 mL 1.0029 mL 2.0058 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
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    体内:

    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

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    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.
    純度とドキュメンテーション

    純度: 99.85%

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

    取扱説明書 (2659 KB)
    参考文献
    動物実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    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
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Avapritinib Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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

    最近チェックした製品:

    オンラインお問い合わせ

    Your information is safe with us. * Required Fields.

    製品名

    		  

    カスタマ需要量 *

    お名前 *

    		 

    タイトル

    メールアドレス *

    		 

    電話番号 *

    デパートメント

    		 

    組纖名 *

    市区町村

    都道府県

    国或いは地域 *

    		      

    必ず会社名を記載ください。個人への返信は行いません。

    備考

    バルクお問い合わせ

    Inquiry Information

    製品名:
    Avapritinib
    製品番号:
    HY-101561
    数量:
    MCE 日本正規代理店:

    カスタマーレビュー

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    製品名

    		  

    Lot #

    お名前 *

    		 

    メールアドレス *

    電話番号 *

    		 

    部門 *

    組纖名 *

    		 

    国或いは地域 *

    備考

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.