[CAS NO. 445430-58-0] BMS-345541

Name: BMS-345541
Brand: Arctom Scientific
SKU: AS938902

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [445430-58-0]

Distributor

Catalog

AS938902

Brand

Arctom Scientific

CAS

445430-58-0

DESCRIPTION [445430-58-0]

Overview

MDL	MFCD18089812
Molecular Weight	255.32
Molecular Formula	C14H17N5
SMILES	CC1=CN=C2C(NCCN)=NC3=CC=C(C)C=C3N21

For research use only. We do not sell to patients.

15 Publications Citing Use of MCE

Summary

BMS-345541 is a selective inhibitor of the catalytic subunits of IKK ( IKK-2 IC ₅₀ =0.3 μM, IKK-1 IC ₅₀ =4 μM). BMS-345541 binds at an allosteric site of IKK .

IC50 & Target

IKK-2

0.3 μM (IC ₅₀ )

IKK-1

4 μM (IC ₅₀ )

In Vitro

BMS-345541 selectively inhibits the stimulated phosphorylation of IκBα in cells (IC ₅₀ =4 μM). Consistent with the role of IKK/NF-κB in the regulation of cytokine transcription, BMS-345541 inhibits lipopolysaccharide-stimulated tumor necrosis factor α, interleukin-1β, interleukin-8, and interleukin-6 in THP-1 cells with IC ₅₀ values in the 1 to 5 μM range ^[1] . BMS-345541 treatment results in a concentration-dependent inhibition of melanoma cell proliferation in SK-MEL-5, A375, and Hs 294T cells. BMS-345541 (0, 100 μM) shows apoptotic features as revealed by TUNEL staining and nuclear condensation ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

BMS-345541 (10 mg/kg, p.o.) results in prolonged serum drug levels, with concentrations sustained at or above 1 μM for many hours in mice. BMS-345541 dose-dependently inhibits the production of TNFα measured in the serum of animals challenged with an intraperitoneal administration of LPS ^[1] . BMS-345541 (0, 10, 25, and 75 mg/kg, p.o.) effectively inhibits SK-MEL-5 tumor growth in a dose-dependent manner in the mice. Tumor-bearing mice treated with 75 mg/kg of BMS-345541 show effective inhibition of growth of SK-MEL-5, A375, and Hs 294T tumors by 86±2.8%, 69±11% and 67±3.4%, respectively ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 10 mg/mL ( 39.17 mM ; Need ultrasonic)

H ₂ O : 10 mg/mL ( 39.17 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.9167 mL	19.5833 mL	39.1665 mL
5 mM	0.7833 mL	3.9167 mL	7.8333 mL
10 mM	0.3917 mL	1.9583 mL	3.9167 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 1 mg/mL (3.92 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1 mg/mL (3.92 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 1 mg/mL (3.92 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

1,2-Ethanediamine, N¹-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)-

1,2-Ethanediamine, N-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)-

N¹-(1,8-Dimethylimidazo[1,2-a]quinoxalin-4-yl)-1,2-ethanediamine