ChemicalBook--->CAS DataBase List--->946518-61-2

946518-61-2

946518-61-2 Structure

946518-61-2 Structure
IdentificationBack Directory
[Name]

LY2409881
[CAS]

946518-61-2
[Synonyms]

2-[5-Chloro-2-[[3-(4-methyl-1-piperazinyl)propyl]amino]-4-pyrimidinyl]-N-cyclopropylbenzo[b]thiophene-4-carboxamide
2-(5-chloro-2-((3-(4-methylpiperazin-1-yl)propyl)amino)pyrimidin-4-yl)-N-cyclopropylbenzo[b]thiophene-4-carboxamide
2-{5-chloro-2-[3-(4-methyl-piperazin-1-yl)-propylamino]-pyrimidin-4-yl}-benzo[b]thiophene-4-carboxylic acid cyclopropylamide
[Molecular Formula]

C24H29ClN6OS
[MOL File]

946518-61-2.mol
[Molecular Weight]

485.04
Chemical PropertiesBack Directory
[density ]

1.37±0.1 g/cm3(Predicted)
[pka]

14.17±0.20(Predicted)
Safety DataBack Directory
[Symbol(GHS) ]

Exclamation Mark (GHS07)
GHS07
[Signal word ]

Warning
[Hazard statements ]

H302
[Precautionary statements ]

P280-P305+P351+P338
Hazard InformationBack Directory
[Uses]

LY2409881 is a selective IκB kinase β (IKK2) inhibitor with an IC50 of 30 nM.
[in vivo]

A well-established xenograft model of DLBCL is used to confirm the activity of LY2409881 in vivo. SCID-beige mice implanted with LY10 cell-derived tumors are given intraperitoneal injections of LY2409881 twice weekly at three different doses: 50, 100, and 200 mg/kg. The treatments are well tolerated, resulting in no death or severe morbidity of the mice. The average tumor volume is graphed as a function of time for each treatment group. The rates of tumor volume growth of the treatment groups are all significantly slower than the untreated control group (P≤0.01)[1].

[IC 50]

IKK2: 30 nM (IC50)
[References]

[1] Deng C, 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 Jan 1;21(1):134-45. DOI:10.1158/1078-0432.CCR-14-0384
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