Quality Control of 1,5-Dibromopentane. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 1,5-Dibromopentane, is researched, Molecular C5H10Br2, CAS is 111-24-0, about Discovery of M-1121 as an Orally Active Covalent Inhibitor of Menin-MLL Interaction Capable of Achieving Complete and Long-Lasting Tumor Regression. Author is Zhang, Meng; Aguilar, Angelo; Xu, Shilin; Huang, Liyue; Chinnaswamy, Krishnapriya; Sleger, Taryn; Wang, Bo; Gross, Stefan; Nicolay, Brandon N.; Ronseaux, Sebastien; Harvey, Kaitlin; Wang, Yu; McEachern, Donna; Kirchhoff, Paul D.; Liu, Zhaomin; Stuckey, Jeanne; Tron, Adriana E.; Liu, Tao; Wang, Shaomeng.
Targeting the menin-MLL protein-protein interaction is being pursued as a new therapeutic strategy for the treatment of acute leukemia carrying MLL-rearrangements (MLLr leukemia). Herein, we report M-1121(I), a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression. M-1121 (I) establishes covalent interactions with Cysteine 329 located in the MLL binding pocket of menin and potently inhibits growth of acute leukemia cell lines carrying MLL translocations with no activity in cell lines with wild-type MLL. Consistent with the mechanism of action, M-1121 (I) drives dose-dependent down-regulation of HOXA9 and MEIS1 gene expression in the MLL-rearranged MV4;11 leukemia cell line. M-1121 (I) is orally bioavailable and shows potent antitumor activity in vivo with tumor regressions observed at tolerated doses in the MV4;11 s.c. and disseminated models of MLL-rearranged leukemia. Together, our findings support development of an orally active covalent menin inhibitor as a new therapy for MLLr leukemia.
This literature about this compound(111-24-0)Quality Control of 1,5-Dibromopentanehas given us a lot of inspiration, and I hope that the research on this compound(1,5-Dibromopentane) can be further advanced. Maybe we can get more compounds in a similar way.
Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis