2. Epigenetics Apoptosis
  3. Epigenetic Reader Domain Apoptosis
  4. VTP50469

VTP50469  (Synonyms: SNDX-50469)

製品番号: HY-114162 純度: 99.70%
COA 取扱説明書 Technical Support

VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 has potently anti-leukemia activity.

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CAS 番号 : 2169916-18-9

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 625 在庫あり
Solution
10 mM * 1 mL in DMSO USD 625 在庫あり
Solid
1 mg $214 在庫あり
5 mg $450 在庫あり
10 mg $540 在庫あり
25 mg $805 在庫あり
50 mg $960 在庫あり
100 mg $1300 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 11 publication(s) in Google Scholar

Other Forms of VTP50469:

VTP50469 関連抗体

Top Publications Citing Use of Products

    VTP50469 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Mar 18;16(1):2641.  [Abstract]

    Relative viability of MOLM-13 cells following treatment with different concentrations of VTP50469 (3.91-1000 nM) over 2-7 days.

    VTP50469 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Mar 18;16(1):2641.  [Abstract]

    Relative viability of human AML cell lines upon treatment with different concentrations of VTP50469 (3.91-1000 nM) over 5 days.

    VTP50469 purchased from MedChemExpress. Usage Cited in: Leukemia. 2025 Jan;39(1):75-86.  [Abstract]

    NPM1::CCDC28A cells and mouse cKit+ bone marrow cells were incubated with selinexor or VTP50469 (0, 0.1, 0.3, 1, 3, 10, and 30 μM) at the indicated concentration for 72 h. Cell viability was assessed using the Cell Counting Kit-8.

    VTP50469 purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2023 Sep;25(9):1346-1358.  [Abstract]

    Immunoblot analysis of 1014 Kdm6a isogenic cells treated with inhibitors that block the function of epigenetic modifiers that normally maintain gene expression including VTP50469 (500 nM), EPZ-5676 (1 μM), PF-9363 (100 nM), JQAD1 or DMSO for 6 days.

    VTP50469 purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2022 Jan 11;12(1):5.  [Abstract]

    A, B MOLM13 and OCI-AML3 cells were treated with the indicated concentrations of VTP50469 (SNDX-50469; 0, 0.25, 1 μM) for 48 h. Following this, total cell lysates were prepared and immunoblot analyses were conducted. The expression levels of β-Actin in the lysates served as the loading control.

    Epigenetic Reader Domain 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
    Brd BRPF1 BRPF2 BRPF3 BRD2 BRD3 BRD4 BRDT CECR2 BD1 BD2 BRD7 BRD9 BET BAZ

    • 生物活性

    • 純度とドキュメンテーション

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    製品説明

    VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 has potently anti-leukemia activity[1][2].

    IC50 & Target

    Ki: 104 pM (Menin-MLL interaction)[1][2]
    Cellular Effect
    Cell Line Type Value Description References
    MOLM-13 GI50
    13 nM
    Compound: 12; VTP50469
    Antiproliferative activity against human MOLM-13 cells
    Antiproliferative activity against human MOLM-13 cells
    		[PMID: 34726905]
    MV4-11 GI50
    17 nM
    Compound: 12; VTP50469
    Antiproliferative activity against human MV4-11 cells
    Antiproliferative activity against human MV4-11 cells
    		[PMID: 34726905]
    体外実験

    VTP50469 more potently and rapidly inhibits cell proliferation in a concentration-dependent manner in MLL-r cell lines carrying (MOLM13 (IC50 of 13 nM), THP1 (IC50 of 37 nM), NOMO1 (IC50 of 30 nM), ML2 (IC50 of 16 nM), EOL1 (IC50 of 20 nM), and murine MLL-AF9 cells (IC50 of 15 nM)) and ALL (KOPN8 (IC50 of 15 nM), HB11;19 (IC50 of 36 nM), MV4;11 (IC50 of 17 nM), SEMK2 (IC50 of 27 nM), and RS4;11 (IC50 of 25 nM)) cell lines[1].
    At early timepoints MLL-r B cell ALL (B-ALL) cell lines, but not MLL-r AML cell lines, underwent apoptosis in response to VTP50469 in a dose-dependent manner. MLL-r AML cell lines underwent dose-dependent differentiation starting at 4-6 days of exposure to VTP50469[1].
    VTP50469 displaces Menin from protein complexes and inhibits chromatin occupancy of MLL at select genes. Loss of MLL binding led to changes in gene expression, differentiation, and apoptosis[1].

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

    VTP50469 関連抗体
    体内実験

    VTP50469 (15-60 mg/kg; oral administration; twice a day; for 28 days; NSG mice) treatment is highly efficacious across all dosage levels and all treatment groups have a significant survival advantage. Mice dosed at 30 and 60 mg/kg VTP50469 extends survival advantage[1].

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

    Animal Model: Unconditioned immunodeficient (NSG) mice with MV4;11 cells[1]
    Dosage: 15 mg/kg, 30 mg/kg, and 60 mg/kg
    Administration: Oral administration; twice a day; for 28 days
    Result: Was highly efficacious across all dosage levels and all treatment groups had a significant survival advantage over the control group.
    分子量

    630.82

    分子式

    C32H47FN6O4S
    CAS 番号
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(N(C(C)C)C(C)C)C1=CC(F)=CC=C1OC2=CN=CN=C2N3CC4(CCN(C[C@H]5CC[C@H](NS(=O)(C)=O)CC5)CC4)C3
    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 : 100 mg/mL (158.52 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 1.5852 mL 7.9262 mL 15.8524 mL
    5 mM 0.3170 mL 1.5852 mL 3.1705 mL
    10 mM 0.1585 mL 0.7926 mL 1.5852 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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    Volume
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    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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (3.96 mM); Clear solution

    • Protocol 2

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (3.96 mM); Clear solution

    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: 99.70%

    COA (253 KB)

    取扱説明書 (2659 KB)
    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, 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 1.5852 mL 7.9262 mL 15.8524 mL 39.6310 mL
    5 mM 0.3170 mL 1.5852 mL 3.1705 mL 7.9262 mL
    10 mM 0.1585 mL 0.7926 mL 1.5852 mL 3.9631 mL
    15 mM 0.1057 mL 0.5284 mL 1.0568 mL 2.6421 mL
    20 mM 0.0793 mL 0.3963 mL 0.7926 mL 1.9815 mL
    25 mM 0.0634 mL 0.3170 mL 0.6341 mL 1.5852 mL
    30 mM 0.0528 mL 0.2642 mL 0.5284 mL 1.3210 mL
    40 mM 0.0396 mL 0.1982 mL 0.3963 mL 0.9908 mL
    50 mM 0.0317 mL 0.1585 mL 0.3170 mL 0.7926 mL
    60 mM 0.0264 mL 0.1321 mL 0.2642 mL 0.6605 mL
    80 mM 0.0198 mL 0.0991 mL 0.1982 mL 0.4954 mL
    100 mM 0.0159 mL 0.0793 mL 0.1585 mL 0.3963 mL
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    VTP50469 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:

    VTP504692169916-18-9SNDX-50469VTP 50469VTP-50469SNDX50469SNDX 50469Epigenetic Reader DomainApoptosisMenin-MLLprotein-proteinleukemiaantiproliferativedifferentiationapoptosissurvivalInhibitorinhibitorinhibit

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    製品番号:
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