BRD7116

Names

[ Name ]:
BRD7116

[Synonym ]:
Cyclopropanecarboxamide, N,N'-(sulfonyldi-4,1-phenylene)bis[2,2,3,3-tetramethyl-
N,N'-(Sulfonyldi-4,1-phenylene)bis(2,2,3,3-tetramethylcyclopropanecarboxamide)
BRD7116

Biological Activity

[Description]:

BRD7116 competitively binds to bacterial DNA gyrase, exhibits an EC50 of 200 nM for LSCe cells, with cell-non-autonomous anti-leukemia activity.IC50 value: 200 nM (EC50, for LSCe cells)Target: DNA gyraseBRD7116 is a bis-aryl sulfone, shows evidence of stroma-mediated anti-LSCe activity. BRD7116 exhibits an EC50 of 200 nM for LSCe cells in co-culture, whereas it displays limited activity against normal HSPCs and AML cell lines (~50% inhibition at 20 μM). BRD7116 also shows activity against patient-derived, primary human leukemia cells. [1] BRD7116 inhibits LSCs via non-cell-autonomous effects on stromal cells as well as cell-autonomous induction of myeloid differentiation genes in LSCs.

[Related Catalog]:

Signaling Pathways >> Others >> Others

Research Areas >> Others

[References]

[1]. Hartwell KA, et al. Niche-based screening identifies small-molecule inhibitors of leukemia stem cells. Nat Chem Biol. 2013 Dec;9(12):840-848

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
681.1±40.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₈H₃₆N₂O₄S

[ Molecular Weight ]:
496.661

[ Flash Point ]:
365.7±27.3 °C

[ Exact Mass ]:
496.239563

[ LogP ]:
6.40

[ Vapour Pressure ]:
0.0±2.1 mmHg at 25°C

[ Index of Refraction ]:
1.576

[ Storage condition ]:
2-8℃

Safety Information

[ RIDADR ]:
NONH for all modes of transport