2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. AZD9496 maleate

AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).

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

AZD9496 maleate Chemical Structure

AZD9496 maleate Chemical Structure

CAS No. : 1639042-28-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 147 In-stock
Solution
10 mM * 1 mL in DMSO USD 147 In-stock
Solid
2 mg USD 70 In-stock
5 mg USD 120 In-stock
10 mg USD 200 In-stock
50 mg USD 700 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 27 publication(s) in Google Scholar

Other Forms of AZD9496 maleate:

AZD9496 maleate Related Antibodies

Top Publications Citing Use of Products

    AZD9496 maleate purchased from MedChemExpress. Usage Cited in: J Nutr Biochem. 2020 Sep;83:108438.  [Abstract]

    AZD9496 suppresses NLRP3 inflammasome activation and assembly in vitro. Protein levels of NLRP3, ASC, Caspase-1, and ERα in colon tissues.

    AZD9496 maleate purchased from MedChemExpress. Usage Cited in: J Nutr Biochem. 2020 Sep;83:108438.  [Abstract]

    AZD9496 suppresses NLRP3 inflammasome activation and assembly in DSS-treated C57BL/6 mice.Colon tissue is immunofluorescently stained with Cy5-NLRP3 antibody, PE-ASC antibody, and FITC-Pro-Caspase-1 antibody.

    AZD9496 maleate purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2019 Jul;52(4):e12612.  [Abstract]

    The expression levels of ERα, DNMT1, ISL1, Ras, Raf1, p‐ERK and ERK are detected by Western blot in MCF-7-OCT4 cells that are treated with AZD9496 (300 nM for 1 h).

    View All Estrogen Receptor/ERR Isoform Specific Products:

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    Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).

    IC50 & Target

    IC50: 0.28 nM (ERα antagonism), 0.14 nM (ERα downregulation), 0.82 nM (ERα binding)[1]
    In Vitro

    The potency of AZD9496 with IC50 of 0.82 nM, 0.14 nM, and 0.28 nM in ERα binding, downregulation, and antagonism, respectively. AZD9496 significantly inhibits MCF-7 cell growth with EC50 of 0.04 nM[1]. Selectivity of AZD9496 over other tested nuclear hormone receptors is high: androgen receptor (AR), IC50=30 μM; glucocorticoid receptor (GR), IC50=9.2 μM; progesterone receptor (PR), IC50=0.54 μM[2].

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

    AZD9496 maleate Related Antibodies
    In Vivo

    Significant tumor growth inhibition is observed as low as 0.5 mg/kg dose in the estrogen-dependent MCF-7 xenograft model, where this effect is accompanied by a dose-dependent decrease in PR protein levels, demonstrating potent antagonist activity. Combining AZD9496 with PI3K pathway and CDK4/6 inhibitors lead to further growth-inhibitory effects compared with monotherapy alone. AZD9496, given once daily orally at 5 and 25 mg/kg produced statistically significant increases in uterine weight compared with the ICI 182780 control (P<0.001) but significantly lower than ICI 47699 (P=0.001)[1]. AZD9496 is also tested in a long-term estrogen deprived model (LTED), using the HCC-1428 LTED cell line that grows in the absence of estrogen and is thought to best represent a model of aromatase inhibition. AZD9496 shows significant activity, with a dose of 5 mg/kg giving tumor regressions in this model[2].

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

    558.55

    Formula

    C29H29F3N2O6
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to brown

    SMILES

    O=C(O)/C=C/C1=CC(F)=C([C@H]2N(CC(C)(F)C)[C@H](C)CC3=C2NC4=C3C=CC=C4)C(F)=C1.O=C(O)/C=C\C(O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (179.04 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 1.7903 mL 8.9517 mL 17.9035 mL
    5 mM 0.3581 mL 1.7904 mL 3.5807 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 (protect from light, stored under nitrogen). 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)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    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: ≥ 2.75 mg/mL (4.92 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.
    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    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
    References
    Cell Assay
    [1]

    Effect of AZD9496, ICI 182780, and ICI 47699 on ERα peptide turnover in MCF-7 cells. Cells are grown in steroid-free conditions in SILAC media containing 13C615N4 L-arginine to label ERα peptide as “heavy” (blue line) and then switched to grow in media containing unlabeled L-arginine to label newly synthesized protein as “normal” (red line) with 0.1% DMSO, 300 nM Tamoxife, 100 nM AZD9496, or 100 nM ICI 182780 for the time indicated. Data shown is representative of two independent experiments[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    In vivo efficacy of AZD9496 in MCF-7 xenograft model. MCF-7 xenografts, grown in male SCID mice, are dosed daily with either PEG/captisol (vehicle) or AZD9496 (0.02, 0.1, 0.5, 10, and 50 mg/kg, p.o., q.d.). Tumor growth is measured by caliper at regular intervals and mean tumor volumes plotted for each dosed group.

    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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). 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 1.7904 mL 8.9518 mL 17.9035 mL 44.7588 mL
    5 mM 0.3581 mL 1.7904 mL 3.5807 mL 8.9518 mL
    10 mM 0.1790 mL 0.8952 mL 1.7904 mL 4.4759 mL
    15 mM 0.1194 mL 0.5968 mL 1.1936 mL 2.9839 mL
    20 mM 0.0895 mL 0.4476 mL 0.8952 mL 2.2379 mL
    25 mM 0.0716 mL 0.3581 mL 0.7161 mL 1.7904 mL
    30 mM 0.0597 mL 0.2984 mL 0.5968 mL 1.4920 mL
    40 mM 0.0448 mL 0.2238 mL 0.4476 mL 1.1190 mL
    50 mM 0.0358 mL 0.1790 mL 0.3581 mL 0.8952 mL
    60 mM 0.0298 mL 0.1492 mL 0.2984 mL 0.7460 mL
    80 mM 0.0224 mL 0.1119 mL 0.2238 mL 0.5595 mL
    100 mM 0.0179 mL 0.0895 mL 0.1790 mL 0.4476 mL
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    AZD9496 maleate 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:

    AZD94961639042-28-6AZD 9496AZD-9496Estrogen Receptor/ERRInhibitorinhibitorinhibit

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