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BAY1238097 

Cat. No.: HY-112316 Purity: 98.53% ee.: 98.06%
Handling Instructions

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).

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

BAY1238097 Chemical Structure

BAY1238097 Chemical Structure

CAS No. : 1564268-08-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 165 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
50 mg USD 950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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).

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, 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 and MM models. BAY 1238097 has in vivo anti-tumour activity in lymphoma models[1][2].
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].

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
Dosage: 15 mg/kg (maximal tolerated dose).
Administration: Orally daily for 12 days (on day 21 post-tumour inoculation).
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].
Storage

4°C, stored under nitrogen

Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (332.18 mM; Need ultrasonic)

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.
In Vivo:
  • 1.

    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

  • 2.

    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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

*All of the co-solvents are provided by MCE.
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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
BAY1238097
Cat. No.:
HY-112316
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BAY1238097

Cat. No.: HY-112316