BAY1238097
Based on 1 Customer Validation
BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50 <100 nM).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.02%
- No. CAS: 1564268-08-1
- Fòrmula: C25H33N5O3
- Peso molecular:451.56
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Almacenamiento:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (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
- Pureza y Documentación
- Referencias
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Help & FAQs
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Epigenetics Compound Library
HY-L005
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Histone Modification Research Compound Library
HY-L024
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Anti-Cancer Compound Library
HY-L025
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Clinical Compound Library
HY-L026
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Reprogramming Compound Library
HY-L039
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Anti-Blood Cancer Compound Library
HY-L079
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Highly Selective Inhibitors Library
HY-L158
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Anti-Hematopathy Compound Library
HY-L171
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Clinical Compound Library Plus
HY-L026P
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Actividad biológica
IC50: < 100 nM (BET in a TR-FRET assay)[1].
BAY 1238097 shows strong inhibitory activity (IC50 < 100 nM) in a TR-FRET assay using BET BRD4 bromodomain 1 and an acetylated peptide derived from histone H4. In the NanoBRET assay, the interaction between BRD4 (IC50=63 nM), BRD3 or BRD2 (IC50=609 nM) and H4 (IC50=2430 nM) is inhibited[1].
BAY 1238097 has in vitro anti-tumour activity in lymphoma models. BAY 1238097 affects the gene expression of GCB DLBCL cells. At the gene level, BTK, CCDC86, CCND2, CD19, CD27, FAIM, FCMR (FAIM3), IL7R, IRAK1, MAPK13, MYB, MYC, PDE4B, TNFRSF13B, TNFRSF17 are among the top downregulated genes. Beside histone-coding genes, the upregulated genes include CCL5, CDKN2C, CD69, JUN, and MKNK2[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
BAY 1238097 is well tolerated at 10-15 mg/kg applied daily over 9-14 days in different disease models, with no obvious toxicity[1][2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Severe combined immunodeficiency (SCID) female mice (9-12 weeks old) inoculated subcutaneously into the right flank with 5×106 SU-DHL-8 cells/mouse suspended in 0.1 mL of matrigel or with O
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Dosage:15 mg/kg (maximal tolerated dose).
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Administration:Orally daily for 12 days (on day 21 post-tumour inoculation).
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Result:Showed strong efficacy in the AML models THP-1, MOLM-13 and KG-1, with T/C between 13 and 20%. Also active in MM models in a human IGH-cyclin D1 translocated MOLP-8 model with a T/C of 3%[2].
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1564268-08-1
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Appearance Solid
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Peso molecular 451.56
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Fòrmula C25H33N5O3
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Color Light yellow to yellow
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SMILES
O=C(N1N=C(C2=CC=C(N3CCN(C)CC3)C=C2)C4=CC(OC)=C(OC)C=C4C[C@@H]1C)NC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvente y solubilidad
DMSO : 150 mg/mL (332.18 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 (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 (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 (5.54 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 (5.54 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. * In solvent : -80°C, 6 months; -20°C, 1 month (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.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 (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 |
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| DMSO | 1 mM | 2.2145 mL | 11.0727 mL | 22.1455 mL | 55.3636 mL |
| 5 mM | 0.4429 mL | 2.2145 mL | 4.4291 mL | 11.0727 mL | |
| 10 mM | 0.2215 mL | 1.1073 mL | 2.2145 mL | 5.5364 mL | |
| 15 mM | 0.1476 mL | 0.7382 mL | 1.4764 mL | 3.6909 mL | |
| 20 mM | 0.1107 mL | 0.5536 mL | 1.1073 mL | 2.7682 mL | |
| 25 mM | 0.0886 mL | 0.4429 mL | 0.8858 mL | 2.2145 mL | |
| 30 mM | 0.0738 mL | 0.3691 mL | 0.7382 mL | 1.8455 mL | |
| 40 mM | 0.0554 mL | 0.2768 mL | 0.5536 mL | 1.3841 mL | |
| 50 mM | 0.0443 mL | 0.2215 mL | 0.4429 mL | 1.1073 mL | |
| 60 mM | 0.0369 mL | 0.1845 mL | 0.3691 mL | 0.9227 mL | |
| 80 mM | 0.0277 mL | 0.1384 mL | 0.2768 mL | 0.6920 mL | |
| 100 mM | 0.0221 mL | 0.1107 mL | 0.2215 mL | 0.5536 mL |
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