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
• Empirical Formula (Hill Notation): C₂₄H₂₉ClN₆OS · xHCl
• Molecular Weight: 485.04 (free base basis)
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD28900675
• Assay: ≥98% (HPLC)
• Form: powder
• Storage condition: desiccated

Properties

• Quality Segment: 100
• 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

Description

Biochem/physiol Actions

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.).

Potent and selective IκB kinase β (IKK2, IKKβ, IKKbeta) inhibitor with in vitro and in vivo anticancer efficacy.

Safety Information

• Storage Class: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable