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BAY1238097

Catalog No. T12660L CAS 1564268-08-1

BAY1238097 is a potent and selective bromodomain and extra-terminal motif (BET) inhibitor with anticancer activity that exhibits strong antiproliferative activity in AML (Acute Myeloid Leukemia) and MM (Multiple Myeloma) models.BAY1238097 can be used for the study of advanced refractory malignancies.

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BAY1238097, CAS 1564268-08-1

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1 mg	In stock	$ 99.00

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Purity: 98.55%

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Description	BAY1238097 is a potent and selective bromodomain and extra-terminal motif (BET) inhibitor with anticancer activity that exhibits strong antiproliferative activity in AML (Acute Myeloid Leukemia) and MM (Multiple Myeloma) models.BAY1238097 can be used for the study of advanced refractory malignancies.
Targets&IC50	BRD4:63 nM, BET:< 100 nM (TR-FRET assay), H4:2430 nM, BRD3(BRD2):609 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

Storage

store under nitrogen

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (221.45 mM), Sonication is recommended.

References and Literature

1. Bernasconi E, et al. Preclinical evaluation of the BET bromodomain inhibitor BAY 1238097 for the treatment of lymphoma. Br J Haematol. 2017 Sep;178(6):936-948. 2. Lejeune, P., et al. (2015) Abstract 3524: BAY 1238097, a novel BET inhibitor with strong efficacy in hematological tumor models. Cancer Research, 75(15 Suppl), 884.

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Keywords

BAY1238097 1564268-08-1 Chromatin/Epigenetic Epigenetic Reader Domain BAY 1238097 BAY-1238097 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.