SML2943
LY2409881 hydrochloride
≥98% (HPLC)
别名:
2-{5-Chloro-2-[3-(4-methylpiperazin-1-yl)propylamino]-pyrimidin-4-yl}benzo[b]thiophene-4-carboxylic acid cyclopropylamide hydrochloride, LY 2409881 hydrochloride, LY-2409881 hydrochloride, N-Cyclopropyl-2-[5-Chloro-2-[[3-(4-methylpiperazin-1-yl)propyl]amino]pyrimidin-4-yl]benzo[b]thiophene-4-carboxamide hydrochloride
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关于此项目
经验公式（希尔记法）:
C24H29ClN6OS · xHCl
分子量:
485.04 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
desiccated
Quality Segment
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
H2O: 2 mg/mL, clear
storage temp.
−20°C
SMILES string
[s]1c2c(c(ccc2)C(=O)NC5CC5)cc1c3nc(ncc3Cl)NCCCN4CCN(CC4)C
InChI key
BNFAYJPQCPZQND-UHFFFAOYSA-N
Biochem/physiol Actions
Potent and selective IκB kinase β (IKK2, IKKβ, IKKbeta) inhibitor with in vitro and in vivo anticancer efficacy.
LY2409881 is a potent IκΒ kinase β (IKK2, IKKβ, IKKbeta) inhibitor (IC50 = 30 nM) that effectively inhibits 10 ng/mL TNFα-induced IκB phosphorylation in LY10 DLBCL cells (by >95%; 10 μM) and exhibits good selectivity by kinase profiling among more than 300 kinases (>10-fold selectivity). LY2409881 enhances TNFα cytotoxicity in SKOV3 ovarian cancer cultures (~20% survival with 316 nM LY2409881 & 10 ng/mL TNFα in 72 hrs; 100% survival with LY2409881 or TNFα alone) by blocking NF-κB antiapoptotic signal activation without affecting TRADD & FADD proapoptotic pathway induction. When administered in vivo, LY2409881 is shown to suppress LY10 xenograft-derived tumor growth in mice (50-200 mg/kg, twice weekly ip.).
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable