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 gyrase BRD7116 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. BRD7116 inhibits LSCs via non-cell-autonomous effects on stromal cells as well as cell-autonomous induction of myeloid differentiation genes in LSCs.
Product information
CAS Number: 329059-55-4
Molecular Weight: 496.66
Formula: C28H36N2O4S
Chemical Name: 2,2,3,3-tetramethyl-N-{4-[4-(2,2,3,3-tetramethylcyclopropaneamido)benzenesulfonyl]phenyl}cyclopropane-1-carboxamide
Smiles: CC1(C)C(C(=O)NC2C=CC(=CC=2)S(=O)(=O)C2C=CC(=CC=2)NC(=O)C2C(C)(C)C2(C)C)C1(C)C
InChiKey: UHXFWAHRAMUDLJ-UHFFFAOYSA-N
InChi: InChI=1S/C28H36N2O4S/c1-25(2)21(26(25,3)4)23(31)29-17-9-13-19(14-10-17)35(33,34)20-15-11-18(12-16-20)30-24(32)22-27(5,6)28(22,7)8/h9-16,21-22H,1-8H3,(H,29,31)(H,30,32)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 48 mg/mL (96.65 mM).
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
References:
- Hartwell KA, et al. Niche-based screening identifies small-molecule inhibitors of leukemia stem cells. Nat Chem Biol. 2013 Dec;9(12):840-848
Products are for research use only. Not for human use.
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