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BAY1238097 

Cat. No.: HY-112316
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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 in a TR-FRET assay).

For research use only. We do not sell to patients.

BAY1238097 Chemical Structure

BAY1238097 Chemical Structure

CAS No. : 1564268-08-1

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  • Biological Activity

  • Protocol

  • Technical Information

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  • References

Description

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 in a TR-FRET assay).

IC50 & Target

IC50: < 100 nM (BET in a TR-FRET assay)[1].

In Vitro

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, 143 probes (121 annotated transcripts) are downregulated and 71 (59 annotated transcripts) are upregulated. 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].

In Vivo

BAY 1238097 shows strong efficacy in the AML models THP-1, MOLM-13 and KG-1, with T/C between 13 and 20%. BAY 1238097 is also active in MM models in a human IGH-cyclin D1 translocated MOLP-8 model with a T/C of 3%. In this model, BAY 1238097 is well tolerated at 10 mg/kg applied over 14 days, with no body weight loss measured. BAY 1238097 is also active against the FGFR/MMSET translocated model NCIH929, with 19% T/C versus 49% T/C for the standard-of-care lenalidomide. BAY 1238097 is well tolerated applied at 12 mg/kg for 9 days (maximum body weight loss 6%)[1]. BAY 1238097 has in vivo anti-tumour activity in lymphoma models[2].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2145 mL 11.0727 mL 22.1455 mL
5 mM 0.4429 mL 2.2145 mL 4.4291 mL
10 mM 0.2215 mL 1.1073 mL 2.2145 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[2]

Mice[2]
Severe combined immunodeficiency (SCID) female mice (9-12 weeks old) are inoculated subcutaneously into the right flank with 5×106 SU-DHL-8 cells/mouse suspended in 0.1 mL of matrigel or with OCI-LY-3 tumour fragments (3×3 mm). BAY 1238097 is administered orally at 10 mL/kg. Treatments with BAY 1238097 or vehicle control are initiated on day 4 post tumour inoculation for the SU-DHL-8 model (8 mice/group). BAY 1238097 is applied daily for 12 days at its maximal tolerated dose (MTD) of 15 mg/kg. Treatment of the OCI-LY-3 tumours start on day 21 post-tumour inoculation, with mice being randomized with a median tumour size per group of 98 mm3 for the BAY 1238097-treated group (n=7) and 93 mm3 for the vehicle control group (n=8). BAY 1238097 is applied at the MTD of 45 mg/kg using an intermittent schedule, twice a week, for 4 weeks[2].

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

References
Molecular Weight

451.56

Formula

C₂₅H₃₃N₅O₃

CAS No.

1564268-08-1

SMILES

O=C(N1N=C(C2=CC=C(N3CCN(C)CC3)C=C2)C4=CC(OC)=C(OC)C=C4C[[email protected]@H]1C)NC

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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BAY1238097
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HY-112316
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BAY1238097

Cat. No.: HY-112316