| Identification | Back Directory | [Name]
BAY1238097 | [CAS]
1564268-08-1 | [Synonyms]
BAY1238097
BAY1238097,BAY-1238097
3H-2,3-Benzodiazepine-3-carboxamide, 4,5-dihydro-7,8-dimethoxy-N,4-dimethyl-1-[4-(4-methyl-1-piperazinyl)phenyl]-, (4S)- | [Molecular Formula]
C25H33N5O3 | [MDL Number]
MFCD31807603 | [MOL File]
1564268-08-1.mol | [Molecular Weight]
451.56 |
| Chemical Properties | Back Directory | [density ]
1.22±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 150 mg/mL (332.18 mM) | [form ]
Solid | [pka]
15.43±0.60(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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 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].
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| [References]
[1] 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.
[2] 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. DOI:10.1111/bjh.14803 |
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| Company Name: |
InvivoChem
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| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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