AZD9496
Based on 29 publication(s) in Google Scholar
AZD9496 is an effective, selective estrogen receptor (ERα) antagonist with an IC50 of 0.28 nM. AZD9496 is an orally active, selective estrogen receptor degrader (SERD).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.28%
- No. CAS: 1639042-08-2
- Fòrmula: C25H25F3N2O2
- Peso molecular:442.47
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Almacenamiento:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) AZD9496
More- Cancer Res. 2017 Oct 15;77(20):5602-5613. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Cell Mol Biol Lett. 2025 Nov 13;30(1):136. [Abstract]
- Cell Commun Signal. 2019 Aug 14;17(1):94. [Abstract]
- Oncogene. 2018 Aug;37(33):4581-4598. [Abstract]
- NPJ Breast Cancer. 2022 Mar 10;8(1):31. [Abstract]
- Cell Prolif. 2019 Jul;52(4):e12612. [Abstract]
- Mol Cancer Ther. 2020 Jul;19(7):1395-1405. [Abstract]
- J Agric Food Chem. 2021 Dec 8;69(48):14544-14556. [Abstract]
- Ecotoxicol Environ Saf. 2021 Apr 1:212:111991. [Abstract]
- Eur J Pharmacol. 2022 Jun 5;924:174939. [Abstract]
- Eur J Pharmacol. 2021 Dec 15:913:174644. [Abstract]
- Int Immunopharmacol. 2021 May:94:107370. [Abstract]
- Arthritis Res Ther. 2022 Nov 2;24(1):247. [Abstract]
- Chem Biol Interact. 2021 Sep 25:347:109616. [Abstract]
- J Nutr Biochem. 2020 Sep;83:108438. [Abstract]
- Molecules. 2020 Apr 23;25(8):1960. [Abstract]
- Mol Med Rep. 2018 Jun;17(6):7789-7796. [Abstract]
- Sci Rep. 2019 Jun 6;9(1):8341. [Abstract]
- Cell Signal. 2019 Sep:61:86-92. [Abstract]
- Biosci Rep. 2020 Jan 31;40(1):BSR20191330. [Abstract]
- Breast Cancer Res Treat. 2020 Jan;179(1):67-77. [Abstract]
- PLoS One. 2026 May 14;21(5):e0349371. [Abstract]
- Biochem Biophys Res Commun. 2019 Apr 2;511(2):468-475. [Abstract]
- Biochem Biophys Res Commun. 2017 Aug 26;490(3):786-793. [Abstract]
- bioRxiv. 2025 Sep 12.
- Patent. US20240217988A1.
- Harvard University. 2023 Mar. 30487357.
- Research Square Preprint. 2022 May.
Customer Validation & Images
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Actividad biológica
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ERα |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
0.49 nM
Compound: AZD9496
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Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition
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[PMID: 33035677] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1639042-08-2
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Appearance Solid
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Peso molecular 442.47
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Fòrmula C25H25F3N2O2
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Color Light yellow to brown
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (29)
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Journal Impact Factor
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Most Recent
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Cancer Res
Structurally Novel Antiestrogens Elicit Differential Responses from Constitutively Active Mutant Estrogen Receptors in Breast Cancer Cells and Tumors. [Abstract]2017 Oct 15;77(20):5602-5613. PMID: 28904064 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Cell Mol Biol Lett
E0703 targets ERβ to facilitate the upregulation of GLI3, thereby alleviating irradiation-induced DNA damage on lymphocytes. [Abstract]2025 Nov 13;30(1):136. PMID: 41233737 -
Cell Commun Signal
Increased HERV-E clone 4-1 expression contributes to DNA hypomethylation and IL-17 release from CD4+ T cells via miR-302d/MBD2 in systemic lupus erythematosus. [Abstract]2019 Aug 14;17(1):94. PMID: 31412880 -
Oncogene
Proteomic profiling identifies key coactivators utilized by mutant ERα proteins as potential new therapeutic targets. [Abstract]2018 Aug;37(33):4581-4598. PMID: 29748621 -
NPJ Breast Cancer
Estrogen receptor inhibition mediates radiosensitization of ER-positive breast cancer models. [Abstract]2022 Mar 10;8(1):31. PMID: 35273179 -
Cell Prolif
ERα is required for suppressing OCT4-induced proliferation of breast cancer cells via DNMT1/ISL1/ERK axis. [Abstract]2019 Jul;52(4):e12612. PMID: 31012189
AZD9496 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).
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Mol Cancer Ther
The Dysregulated Pharmacology of Clinically Relevant ESR1 Mutants is Normalized by Ligand-activated WT Receptor. [Abstract]2020 Jul;19(7):1395-1405. PMID: 32381587 -
J Agric Food Chem
Estrogen Receptor α Regulates Metabolic-Associated Fatty Liver Disease by Targeting NLRP3-GSDMD Axis-Mediated Hepatocyte Pyroptosis. [Abstract]2021 Dec 8;69(48):14544-14556. PMID: 34817168 -
Ecotoxicol Environ Saf
Effect of bisphenol A on craniofacial cartilage development in zebrafish (Danio rerio) embryos: A morphological study. [Abstract]2021 Apr 1:212:111991. PMID: 33548570 -
Eur J Pharmacol
Estradiol reduced 5-HT reuptake by downregulating the gene expression of Plasma Membrane Monoamine Transporter (PMAT, Slc29a4) through estrogen receptor β and the MAPK/ERK signaling pathway. [Abstract]2022 Jun 5;924:174939. PMID: 35398393 -
Eur J Pharmacol
Syringaresinol attenuates sepsis-induced cardiac dysfunction by inhibiting inflammation and pyroptosis in mice. [Abstract]2021 Dec 15:913:174644. PMID: 34801532 -
Int Immunopharmacol
Isobavachalcone prevents osteoporosis by suppressing activation of ERK and NF-κB pathways and M1 polarization of macrophages. [Abstract]2021 May:94:107370. PMID: 33640858 -
Arthritis Res Ther
PSTPIP2 regulates synovial macrophages polarization and dynamics via ERβ in the joint microenvironment. [Abstract]2022 Nov 2;24(1):247. PMID: 36324152 -
Chem Biol Interact
Bisphenol A and genistein have opposite effects on adult chicken ovary by acting on ERα/Nrf2-Keap1-signaling pathway. [Abstract]2021 Sep 25:347:109616. PMID: 34363818 -
J Nutr Biochem
Soy isoflavones ameliorate experimental colitis by targeting ERα/NLRP3 inflammasome pathways. [Abstract]2020 Sep;83:108438. PMID: 32563803
AZD9496 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 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.
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Molecules
Apigenin Inhibits Histamine-Induced Cervical Cancer Tumor Growth by Regulating Estrogen Receptor Expression. [Abstract]2020 Apr 23;25(8):1960. PMID: 32340124 -
Mol Med Rep
MicroRNA‑148a inhibition protects against ovariectomy‑induced osteoporosis through PI3K/AKT signaling by estrogen receptor α. [Abstract]2018 Jun;17(6):7789-7796. PMID: 29620276 -
Sci Rep
Modeling the Effect of the Metastatic Microenvironment on Phenotypes Conferred by Estrogen Receptor Mutations Using a Human Liver Microphysiological System. [Abstract]2019 Jun 6;9(1):8341. PMID: 31171849 -
Cell Signal
Estrogen receptor alpha regulates the Wnt/β-catenin signaling pathway in colon cancer by targeting the NOD-like receptors. [Abstract]2019 Sep:61:86-92. PMID: 31121307 -
Biosci Rep
17β-estradiol binding to ERα promotes the progression of prolactinoma through estrogen-response element-induced CaBP-9k up-regulation. [Abstract]2020 Jan 31;40(1):BSR20191330. PMID: 31894842 -
Breast Cancer Res Treat
Pharmacokinetic and pharmacodynamic analysis of fulvestrant in preclinical models of breast cancer to assess the importance of its estrogen receptor-α degrader activity in antitumor efficacy. [Abstract]2020 Jan;179(1):67-77. PMID: 31562570 -
PLoS One
2026 May 14;21(5):e0349371. PMID: 42133665 -
Biochem Biophys Res Commun
Estrogen receptors participate in carcinogenesis signaling pathways by directly regulating NOD-like receptors. [Abstract]2019 Apr 2;511(2):468-475. PMID: 30797557 -
Biochem Biophys Res Commun
Regulation of testicular steroidogenesis by Foxa3 via transcriptional modulation of ERα signaling in type 2 diabetes mellitus (T2DM). [Abstract]2017 Aug 26;490(3):786-793. PMID: 28645613 -
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Solvente y solubilidad
DMSO : ≥ 104.5 mg/mL (236.17 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.65 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.65 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 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 (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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (287 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Weir HM, et al. AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and ESR1-Mutant Breast Tumors in Preclinical Models. Cancer Res. 2016 Jun 1;76(11):3307-18. [Content Brief]
[2]. De Savi C, et al. Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist. J Med Chem. 2015 Oct 22;58(20):8128-40. [Content Brief]
[3]. Gough SM, et al. Oral Estrogen Receptor PROTAC Vepdegestrant (ARV-471) Is Highly Efficacious as Monotherapy and in Combination with CDK4/6 or PI3K/mTOR Pathway Inhibitors in Preclinical ER+ Breast Cancer Models. Clin Cancer Res. 2024 Aug 15;30(16):3549-3563. [Content Brief]
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 | 2.2600 mL | 11.3002 mL | 22.6004 mL | 56.5010 mL |
| 5 mM | 0.4520 mL | 2.2600 mL | 4.5201 mL | 11.3002 mL | |
| 10 mM | 0.2260 mL | 1.1300 mL | 2.2600 mL | 5.6501 mL | |
| 15 mM | 0.1507 mL | 0.7533 mL | 1.5067 mL | 3.7667 mL | |
| 20 mM | 0.1130 mL | 0.5650 mL | 1.1300 mL | 2.8251 mL | |
| 25 mM | 0.0904 mL | 0.4520 mL | 0.9040 mL | 2.2600 mL | |
| 30 mM | 0.0753 mL | 0.3767 mL | 0.7533 mL | 1.8834 mL | |
| 40 mM | 0.0565 mL | 0.2825 mL | 0.5650 mL | 1.4125 mL | |
| 50 mM | 0.0452 mL | 0.2260 mL | 0.4520 mL | 1.1300 mL | |
| 60 mM | 0.0377 mL | 0.1883 mL | 0.3767 mL | 0.9417 mL | |
| 80 mM | 0.0283 mL | 0.1413 mL | 0.2825 mL | 0.7063 mL | |
| 100 mM | 0.0226 mL | 0.1130 mL | 0.2260 mL | 0.5650 mL |
AZD9496 Related Classifications
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