LY2409881 trihydrochloride

This product is for research use only, not for human use. We do not sell to patients.

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250mg	$1020	Check With Us
500mg	$1550	Check With Us
1g	$2325	Check With Us

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Cat #: V0757 CAS #: 946518-60-1 Purity ≥ 98%

Description: LY2409881 trihydrochloride (LY-2409881; LY 2409881), the trihydrochloride salt of LY-2409881, is a novel, potent and selective IKK2 ( IκB kinase β) inhibitor with potential anticancer and anti-inflammatory activity.

References: 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.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	594.43
Molecular Formula	C24H32Cl4N6OS
CAS No.	946518-60-1
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 20 mg/mL (33.6 mM)r
	Water: <1 mg/mLr
	Ethanol: <1 mg/mL
Solubility In Vivo	2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5 mg/mL
SMILES Code	O=C(C1=C(C=C(C2=NC(NCCCN3CCN(C)CC3)=NC=C2Cl)S4)C4=CC=C1)NC5CC5.[H]Cl.[H]Cl.[H]Cl
Synonyms	LY2409881 tri-HCl; LY-2409881; LY 2409881; LY2409881 trihydrochloride

Protocol	In Vitro	LY2409881 is an IKK2 inhibitor that inhibits TNFα-induced activation of NF-κB. By in vitro kinase assay, LY2409881 potently inhibits IKK2, with an IC50 of 30 nM. In contrast, the IC50 for IKK1 and other common kinases is at least one log higher. The specificity of LY2409881 for NF-κB signaling is further studied in a cell-based assay, by examining the effect of LY2409881 in the TNFα-dependent antiapoptosis function. TNFα is a well-characterized upstream stimulus of NF-κB. In the ovarian cancer cell line SKOV3, LY2409881 demonstrates moderate cytotoxicity, whereas TNFα at 10 ng/mL does not cause any cytotoxicity. In contrast, coadministration of LY2409881 and TNFα results in markedly higher cell killing compared with LY2409881. This is because TNFα-dependent activation of antiapoptotic signals mediated by NF-κB is blocked by LY2409881, while the proapoptotic TNF receptor-associated death domain (TRADD) and FAS-associated death domain (FADD) cascade pathways activated by TNFα are not affected by LY2409881.
Protocol	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).

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	1.6823 mL	8.4114 mL	16.8228 mL	33.6457 mL
5mM	0.3365 mL	1.6823 mL	3.3646 mL	6.7291 mL
10mM	0.1682 mL	0.8411 mL	1.6823 mL	3.3646 mL
20mM	0.0841 mL	0.4206 mL	0.8411 mL	1.6823 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.