LY2409881
LY2409881 Basic information
- Product Name:
- LY2409881
- 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
- Benzo[b]thiophene-4-carboxamide, 2-[5-chloro-2-[[3-(4-methyl-1-piperazinyl)propyl]amino]-4-pyrimidinyl]-N-cyclopropyl-
- CAS:
- 946518-61-2
- MF:
- C24H29ClN6OS
- MW:
- 485.04
- Mol File:
- 946518-61-2.mol
LY2409881 Chemical Properties
- Density
- 1.37±0.1 g/cm3(Predicted)
- pka
- 14.17±0.20(Predicted)
LY2409881 Usage And Synthesis
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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