AZD5153
Based on 5 publication(s) in Google Scholar
AZD5153 is a bivalent, selective, and orally active BET/BRD4 bromodomain inhibitor with an IC50 of value of 5 nM for full-length BRD4 (FL-BRD4). AZD5153 ligates two bromodomains in BRD4 simultaneously. AZD5153 can be used for the study of cancer, such as acute myeloid leukemia, multiple myeloma, and diffuse large B-cell lymphoma.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.20%
- CAS 番号: 1869912-39-9
- 分子式: C25H33N7O3
- 分子量:479.57
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Epigenetics Compound Library
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Histone Modification Research Compound Library
HY-L024
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HY-L025
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HY-L039
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Orally Active Compound Library
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HY-L077
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Anti-Blood Cancer Compound Library
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Highly Selective Inhibitors Library
HY-L158
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Highly Selective Activators Library
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Cell Death Library
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
生物活性
AZD5153 demonstrates a remarkable enhancement in potency for the displacement of full-length BRD4 relative to BD1, with IC50 values of 5.0 nM and 1.6 µM, for FL-BRD4 and BD1 domain alone (BD1-BRD4) , respectively. AZD5153 demonstrated a drastically reduced IC50 value of 1.4 µM in displacing mutant BRD4 from chromatin, in contrast to 8.7 nM IC50 for wild-type protein[1].
AZD5153 (5.4 nM; 16 h) in MM.1S cells reduces MYC protein levels via flow cytometry[1].
AZD5153 (GI50 <150 nM; 72 h) in 61 hematologic cancer cell lines (AML, MM, DLBCL) inhibits cell growth[1].
AZD5153 (100 nM; 48 h) in MV-4-11 and MM.1S cells induces significant apoptosis via caspase-3 activation, unlike I-BET762[1].
AZD5153 (200 nM; 24 h) in hematologic cell lines (AML, MM, DLBCL) modulates MYC, E2F, and mTOR transcriptional programs via RNA-seq.
AZD5153 (200 nM; 24 h) in sensitive hematologic cell lines (MOLP8, MV-4-11, OCILY19) downregulates mTOR pathway proteins (p-p70S6K, PRAS40, p-4EBP1) via RPPA and western blot[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV-4-11, MM.1S, K562 cells
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Concentration:100 nM
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Incubation Time:48 h
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Result:Induced substantial apoptosis (caspase-3 positive cells).
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Cell Line:AML (KG1A, MOLM13, MV-4-11, OCIAML2), MM (IM9, MM.1S, MOLP8, OPM2, RPMI8226), DLBCL (OCILY19, WILL2)
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Concentration:200 nM
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Incubation Time:24 h
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Result:RNA-seq identified 172 differentially expressed genes, with MYC, E2F, and mTOR pathways significantly downregulated.
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Cell Line:K562 (resistant), IM9 (resistant), MOLP8 (sensitive), MV-4-11 (sensitive), OCILY19 (sensitive)
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Concentration:200 nM
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Incubation Time:24 h
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Result:Showed sensitive cell lines had marked decreases in mTOR pathway proteins (p-p70S6K, PRAS40, p-4EBP1), while MYC was modulated in all lines.
AZD5153 (6.4-12.8 mg/kg/week; subcutaneous mini-pump; continuous; 14 days) in MV-4-11 xenograft mice achieves near-complete tumor regression with prolonged BRD4 inhibition[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female CB17 SCID mice implanted with MV-4-11 (AML) cells[1].
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Dosage:1, 2.5, 5 mg/kg
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Administration:Oral gavage, daily, 14-28 days.
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Result:Oral dosing at 5 mg/kg daily induced tumor regression in MV-4-11 (AML).
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Animal Model:Female SCID beige mice implanted with KMS11 (MM) cells[1].
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Dosage:1, 2.5, 5 mg/kg
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Administration:Oral gavage, daily, 14-28 days.
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Result:Oral dosing at 5 mg/kg daily induced tumor regression in KMS11 (MM) xenografts.
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Animal Model:Female NSG mice implanted with KARPAS422 (DLBCL) cells[1].
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Dosage:1, 2.5, 5 mg/kg
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Administration:Oral gavage, daily, 14-28 days
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Result:Oral dosing at 5 mg/kg daily induced tumor regression in KARPAS422 (DLBCL) xenografts.
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Animal Model:Female CB17 SCID mice implanted with MV-4-11 (AML) cells[1].
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Dosage:6.4, 12.8 mg/kg/week
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Administration:Subcutaneous mini-pump infusion, continuous, 14 days
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Result:Continuous mini-pump delivery at 6.4 mg/kg/week caused tumor stasis, while 12.8 mg/kg/week led to near-complete regression (97%) of MV-4-11 tumors, associated with increased apoptosis and prolonged BRD4 inhibition.
化学情報
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CAS 番号 1869912-39-9
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性状 Solid
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分子量 479.57
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分子式 C25H33N7O3
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Color Off-white to yellow
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SMILES
O=C1N(C)CCN(CCOC2=CC=C(C3CCN(C4=NN5C(C=C4)=NN=C5OC)CC3)C=C2)[C@@H]1C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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J Med Chem
Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib. [Abstract]2020 Jul 9;63(13):7186-7210. PMID: 32453591 -
Mol Cancer Ther
Harnessing senolytics and PARP inhibition to expand the antitumor activity of CDK4/6 inhibitors in prostate cancer. [Abstract]2025 Jul 2. PMID: 40601842 -
Front Cell Dev Biol
AZD5153, a Bivalent BRD4 Inhibitor, Suppresses Hepatocarcinogenesis by Altering BRD4 Chromosomal Landscape and Modulating the Transcriptome of HCC Cells. [Abstract]2022 Mar 24:10:853652. PMID: 35399501 -
J Biomed Mater Res A
Targeting Dysregulated Epigenetic Modifiers With Kidney-Targeted Nanotherapeutics for Polycystic Kidney Disease. [Abstract]2025 Apr;113(4):e37909. PMID: 40200735 -
bioRxiv
2025 Sep 3:2025.08.30.673282. PMID: 40949948
溶剤 & 溶解度
DMSO : 100 mg/mL (208.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (5.21 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 (5.21 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 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.
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.
純度とドキュメンテーション
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データシート (277 KB)
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SDS (396 KB)
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- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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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, 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 |
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| DMSO | 1 mM | 2.0852 mL | 10.4260 mL | 20.8520 mL | 52.1300 mL |
| 5 mM | 0.4170 mL | 2.0852 mL | 4.1704 mL | 10.4260 mL | |
| 10 mM | 0.2085 mL | 1.0426 mL | 2.0852 mL | 5.2130 mL | |
| 15 mM | 0.1390 mL | 0.6951 mL | 1.3901 mL | 3.4753 mL | |
| 20 mM | 0.1043 mL | 0.5213 mL | 1.0426 mL | 2.6065 mL | |
| 25 mM | 0.0834 mL | 0.4170 mL | 0.8341 mL | 2.0852 mL | |
| 30 mM | 0.0695 mL | 0.3475 mL | 0.6951 mL | 1.7377 mL | |
| 40 mM | 0.0521 mL | 0.2607 mL | 0.5213 mL | 1.3033 mL | |
| 50 mM | 0.0417 mL | 0.2085 mL | 0.4170 mL | 1.0426 mL | |
| 60 mM | 0.0348 mL | 0.1738 mL | 0.3475 mL | 0.8688 mL | |
| 80 mM | 0.0261 mL | 0.1303 mL | 0.2607 mL | 0.6516 mL | |
| 100 mM | 0.0209 mL | 0.1043 mL | 0.2085 mL | 0.5213 mL |
AZD5153 関連分類
HY-100653 関連分類
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