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BAY1238097, a potent and selective bromodomain and extra-terminal motif (BET) inhibitor with anticancer activity, exhibits strong antiproliferative effects in AML (Acute Myeloid Leukemia) and MM (Multiple Myeloma) models. BAY1238097 is useful for studying advanced refractory malignancies.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $47 | - | In Stock | |
| 5 mg | $108 | - | In Stock | |
| 10 mg | $185 | - | In Stock | |
| 25 mg | $395 | - | In Stock | |
| 50 mg | $689 | - | In Stock | |
| 100 mg | $1,160 | - | In Stock | |
| 200 mg | $1,560 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $122 | - | In Stock |
| Description | BAY1238097, a potent and selective bromodomain and extra-terminal motif (BET) inhibitor with anticancer activity, exhibits strong antiproliferative effects in AML (Acute Myeloid Leukemia) and MM (Multiple Myeloma) models. BAY1238097 is useful for studying advanced refractory malignancies. |
| Targets&IC50 | H4:2430 nM, BRD3(BRD2):609 nM, BET:< 100 nM (TR-FRET assay), BRD4:63 nM |
| In vitro | BAY 1238097 exhibits potent inhibitory activity (IC50 < 100 nM) in a TR-FRET assay utilizing BET BRD4 bromodomain 1 and an acetylated peptide derived from histone H4. In the NanoBRET assay, it inhibits the interaction between BRD4 (IC50=63 nM), BRD3, or BRD2 (IC50=609 nM), and H4 (IC50=2430 nM)[2]. BAY 1238097 demonstrates in vitro anti-tumor activity in lymphoma models. It influences the gene expression of GCB DLBCL cells. At the gene level, top downregulated genes include BTK, CCDC86, CCND2, CD19, CD27, FAIM, FCMR (FAIM3), IL7R, IRAK1, MAPK13, MYB, MYC, PDE4B, TNFRSF13B, TNFRSF17. In addition to histone-coding genes, upregulated genes include CCL5, CDKN2C, CD69, JUN, and MKNK2[1]. |
| In vivo | BAY 1238097 demonstrates robust efficacy in AML and MM models. It exhibits in vivo anti-tumor activity in lymphoma models[1][2]. BAY 1238097 is well tolerated at doses of 10-15 mg/kg administered daily over 9-14 days in various disease models, with no apparent toxicity[1][2]. |
| Molecular Weight | 451.56 |
| Formula | C25H33N5O3 |
| Cas No. | 1564268-08-1 |
| Smiles | CNC(=O)N1N=C(c2ccc(cc2)N2CCN(C)CC2)c2cc(OC)c(OC)cc2C[C@@H]1C |
| Relative Density. | 1.22 g/cm3 (Predicted) |
| Storage | store under nitrogen,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (221.45 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.86 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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