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Merck
CN

SML2943

LY2409881 hydrochloride

≥98% (HPLC)

Synonym(s):

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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About This Item

Empirical Formula (Hill Notation):
C24H29ClN6OS · xHCl
Molecular Weight:
485.04 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD28900675

Key Documents

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SMILES string

[s]1c2c(c(ccc2)C(=O)NC5CC5)cc1c3nc(ncc3Cl)NCCCN4CCN(CC4)C

InChI key

BNFAYJPQCPZQND-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

H2O: 2 mg/mL, clear

storage temp.

−20°C

Quality Level

100

Related Categories

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.).

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000123039
0000123038
0000105062

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Changchun Deng et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 21(1), 134-145 (2014-10-31)
To evaluate the pharmacologic activity of a novel inhibitor of IκB kinase β (IKK2), LY2409881, in preclinical models of B- and T-cell lymphoma, as a single agent and in combination with histone deacetylase (HDAC) inhibitors. The in vitro activity of
Dong Ren et al.
Molecular cancer, 16(1), 117-117 (2017-07-12)
The primary issue arising from prostate cancer (PCa) is its high prevalence to metastasize to bone, which severely affects the quality of life and survival time of PCa patients. miR-210-3p is a well-documented oncogenic miRNA implicated in various aspects of
Anfernee Kai-Wing Tse et al.
Redox biology, 11, 562-576 (2017-01-21)
Nitrosourea represents one of the most active classes of chemotherapeutic alkylating agents for metastatic melanoma. Treatment with nitrosoureas caused severe systemic side effects which hamper its clinical use. Here, we provide pharmacological evidence that reactive oxygen species (ROS) induction and

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