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  3. AZD9496 maleate

AZD9496 maleate 

Cat. No.: HY-12870A Purity: >95.0%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 221 In-stock
Estimated Time of Arrival: December 31
2 mg USD 96 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 312 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1080 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 18 publication(s) in Google Scholar

Other Forms of AZD9496 maleate:

Top Publications Citing Use of Products

    AZD9496 maleate purchased from MCE. Usage Cited in: Cell Prolif. 2019 Jul;52(4):e12612.

    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).

    AZD9496 maleate purchased from MCE. Usage Cited in: J Nutr Biochem. 2020 Sep;83:108438.

    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 MCE. Usage Cited in: J Nutr Biochem. 2020 Sep;83:108438.

    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.

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    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].

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

    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].

    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.

    1639042-28-6

    SMILES

    O=C(O)/C=C/C1=CC(F)=C([[email protected]]2N(CC(C)(F)C)[[email protected]](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)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" 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
    10 mM 0.1790 mL 0.8952 mL 1.7904 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    *All of the co-solvents are provided by MCE.
    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
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    Keywords:

    AZD9496AZD 9496AZD-9496Estrogen Receptor/ERRInhibitorinhibitorinhibit

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    Product Name:
    AZD9496 maleate
    Cat. No.:
    HY-12870A
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