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).
Product information
CAS Number: 1564268-08-1
Molecular Weight: 451.56
Formula: C25H33N5O3
Chemical Name: (4S)-7,8-dimethoxy-N,4-dimethyl-1-[4-(4-methylpiperazin-1-yl)phenyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide
Smiles: CN1CCN(CC1)C1C=CC(=CC=1)C1=NN([C@@H](C)CC2=CC(OC)=C(C=C12)OC)C(=O)NC
InChiKey: CJIPEACKIJJYED-KRWDZBQOSA-N
InChi: InChI=1S/C25H33N5O3/c1-17-14-19-15-22(32-4)23(33-5)16-21(19)24(27-30(17)25(31)26-2)18-6-8-20(9-7-18)29-12-10-28(3)11-13-29/h6-9,15-17H,10-14H2,1-5H3,(H,26,31)/t17-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 150 mg/mL (332.18 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. 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.
In Vivo:
BAY 1238097 shows strong efficacy in the AML and MM models. BAY 1238097 has in vivo anti-tumour activity in lymphoma models. BAY 1238097 is well tolerated at 10-15 mg/kg applied daily over 9-14 days in different disease models, with no obvious toxicity.
Products are for research use only. Not for human use.
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