1. Membrane Transporter/Ion Channel
  2. Monocarboxylate Transporter
  3. AZD0095

AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib (HY-10205).

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

CAS No. : 2750001-23-9

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

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    AZD0095 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 February 07.

    AZD0095 (1-10 μM). Seahorse metabolic flux assay measured extracellular acidification rate (ECAR) as a function of glycolysis and lactate secretion of PanNET cells in normoxia or hypoxia.

    AZD0095 purchased from MedChemExpress. Usage Cited in: Biosci Rep. 2024 Jul 11:BSR20240752.  [Abstract]

    MCT4 inhibitor AZD0095 (10 μM) increased death level of PC-9 cells induced by SeChry@PUREG4-LA24.

    AZD0095 purchased from MedChemExpress. Usage Cited in: Biosci Rep. 2024 Jul 11:BSR20240752.  [Abstract]

    MCT4 inhibitor AZD0095 (10 μM) decreased death levels of A549 cells and H292 cells induced by SeChry@PUREG4-LA24.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib (HY-10205)[1].

    IC50 & Target[1]

    MCT4

    1.3 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    NCI-H358 GI50
    26 nM
    Compound: 15; AZD0095
    Antiproliferative activity against human NCI-H358 cells assessed as cell growth inhibition
    Antiproliferative activity against human NCI-H358 cells assessed as cell growth inhibition
    [PMID: 36525250]
    In Vitro

    AZD0095 (0-50 µM) inhibits cell proliferation in NCI-H358 cells (high expression of MCT4), with an IC50 of 26 nM[1].

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

    In Vivo

    AZD0095 (100 mg/kg, p.o. bid) together with Cediranib (3 mg/kg, p.o.) reduces tumor growth in a murine NCI-H358 xenograft[1].

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

    Animal Model: Murine NCI-H358 xenograft[1]
    Dosage: 100 mg/kg together with Cediranib (3 mg/kg)
    Administration: Oral administration (p.o.)
    Result: Reduced tumor growth more efficiently than AZD0095 or AZD2171 alone.
    Molecular Weight

    500.60

    Formula

    C27H32N8O2

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    CC1=C(O[C@H]2CN(C3=CC=C(C4=NN=C(CN5CCOCC5)C=C4)C=C3)CC2)C(C)=NC6=NC(C)=NN16

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 10 mg/mL (19.98 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 1.9976 mL 9.9880 mL 19.9760 mL
    5 mM 0.3995 mL 1.9976 mL 3.9952 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • 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: 1 mg/mL (2.00 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1 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 (10.0 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: ≥ 1 mg/mL (2.00 mM); Clear solution

      This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
    Purity & Documentation

    Purity: 99.42%

    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9976 mL 9.9880 mL 19.9760 mL 49.9401 mL
    5 mM 0.3995 mL 1.9976 mL 3.9952 mL 9.9880 mL
    10 mM 0.1998 mL 0.9988 mL 1.9976 mL 4.9940 mL
    15 mM 0.1332 mL 0.6659 mL 1.3317 mL 3.3293 mL
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    • 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.

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    Product Name:
    AZD0095
    Cat. No.:
    HY-148517
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