LY2409881 trihydrochloride

LY2409881 trihydrochloride Basic information
Product Name:LY2409881 trihydrochloride
Synonyms:LY2409881 trihydrochloride;LY2409881;2-(5-chloro-2-(3-(4-methylpiperazin-1-yl)propylamino)pyrimidin-4-yl)-N-cyclopropylbenzo[b]thiophene-4-carboxamide trihydrochloride;2-[5-Chloro-2-[[3-(4-methyl-1-piperazinyl)propyl]amino]-4-pyrimidinyl]-N-cyclopropylbenzo[b]thiophene-4-carboxamide trihydrochloride;LY2409881 triHCl;LY2409881 3HCl;CS-1620;LY-2409881 HC'l
CAS:946518-60-1
MF:C24H30Cl2N6OS
MW:521.51
EINECS:
Product Categories:Inhibitors
Mol File:946518-60-1.mol
LY2409881 trihydrochloride Structure
LY2409881 trihydrochloride Chemical Properties
storage temp. Store at -20°C
solubility ≥59.4 mg/mL in DMSO with ultrasonic; insoluble in EtOH; insoluble in H2O
form solid
Safety Information
MSDS Information
LY2409881 trihydrochloride Usage And Synthesis
Uses2-[5-Chloro-2-[[3-(4-methylpiperazin-1-yl)propyl]amino]pyrimidin-4-yl]benzo[b]thiophene-4-carboxamide N-cyclopropyl Trihydrochloride is an inhibitor of IkB-kinase (IKK2). Small molecules that inhibits IkB-kinase and NF-κB pathways are potential anti-inflammatory drug candidate.
Biological Activityly2409881 is a potent and selective inhibitor of ikk2 with ic50 value of 30 nm [1].iκb kinase β (ikk2) is an enzyme that serves as a subunit of iκb kinase, which is involved in the cytokine-activated immune responses. ikk2 activates nuclear factor kappa-b kinase (nf-κb).ly2409881 is a selective ikk2 inhibitor and exhibited >10-fold selectivity over other common kinases and ikk1. in the ovarian cancer cell line skov3, ly2409881 showed moderate cytotoxicity. while coadministration of ly2409881 and tnfɑ significantly induced cells death, which suggested ly2409881 inhibited nf-κb mediated antiapoptotic signals in a tnfɑ-dependent way. in the dlbcl cell line ly10, ly2409881 (10 μm) inhibited tnfɑ-dependent phosphorylation of iκb. in the dlbcl cell line sudhl2, ly2409881 (10 μm) inhibited the nuclear signals of p50 and nf-κb. also, ly2409881 induced apoptosis in a concentration-dependent way [1].in scid-beige mice bearing ly10 cell-derived tumors, ly2409881 (50, 100 and 200 mg/kg) significantly inhibited tumor growth [1].
references[1]. deng c, lipstein m, rodriguez r, et al. the novel ikk2 inhibitor ly2409881 potently synergizes with histone deacetylase inhibitors in preclinical models of lymphoma through the downregulation of nf-κb. clin cancer res, 2015, 21(1): 134-145.
LY2409881 trihydrochloride Preparation Products And Raw materials
AZD2014 LY 294002 HYDROCHLORIDE Afatinib NS-398 Veliparib Cyclo[Phe-Tyr-Lys(iPr)-D-Arg-2-Nal-Gly-D-Glu]-Lys(iPr)-NH2 (S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide Trametinib LY 88074 Atazanavir sulfate LY-364947 LY 2784544 LY2584702 LY3214996 2-(4-((4-((1-cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)oxy)pyridin-2-yl)amino)pyridin-2-yl)propan-2-ol Etalocib Axitinib LY2228820

Email:[email protected] [email protected]
Copyright © 2024 Mywellwork.com All rights reserved.