[CAS NO. 783348-36-7] MLN120B

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PRODUCTS SPECIFICATIONS [783348-36-7]

Catalog

HY-15473

Brand

MCE

CAS

783348-36-7

DESCRIPTION [783348-36-7]

Overview

MDL	MFCD17392835
Molecular Weight	366.80
Molecular Formula	C19H15ClN4O2
SMILES	O=C(C1=CC=CN=C1C)NC2=C(OC)C(Cl)=CC3=C2NC4=C3C=CN=C4

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

18 Publications Citing Use of MCE

Summary

MLN120B (ML120B) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC ₅₀ of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis ^[1] ^[2] .

IC50 & Target

IKKβ

60 nM (IC ₅₀ )

In Vitro

MLB120B (0-20 μM; 90 minutes) inhibits phosphorylation and degradation of IκB in RPMI 8226 and INA6 cells; however, no significant inhibition is observed in MM.1S cells ^[1] .
MLB120B (1.25-20 μM; 90 minutes) completely abrogates TNF-a-induced phosphorylation and degradation of IκB in a dosedependent fashion. Phosphorylation of p65 NF-κB induced by TNF-a is also blocked by MLN120B ^[1] .
MLN120B inhibits proliferation of multiple myeloma cell lines. MM.1S, MM.1R, RPMI 8226, RPMI-LR5, RPMI-Dox40, U266, and INA6 cells. Five percent to fifty percent and 18% to 70% inhibition in proliferation is observed at doses >20 uM and [ ³ H]thymidine uptake, respectively[1].
MLN120B (1.25-40 μM; 72 hours) almost completely blocks stimulation of MM.1S, U266, and INA6 cell growth, as well as IL-6 secretion from BMSCs, induced by multiple myeloma cell adherence to BMSCs[1].
MLN120B shows an inhibitory effect on LPS induced NF-κB activation in RAW267.4 cells. The IC ₅₀ values of MLN120B is 1.4 µM, 14.8 µM or 27.3 µM for NF-κB2-luc2, IL8-luc2 or TNF-AIP3-luc2 reporter transfected cells, respectively[3].

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

Western Blot Analysis ^[1]

Cell Line:	MM.1S cells
Concentration:	1.25-20 μM
Incubation Time:	90 minutes
Result:	Inhibited p- IκB and p-P65 expression in a dose-dependent manner.

Cell Viability Assay ^[1]

Cell Line:	Multiple myeloma cell lines: MM.1S, MM.1R, RPMI 8226, RPMI-LR5, RPMI-Dox40, U266, and INA6 cells
Concentration:	1.25 μM-20 μM
Incubation Time:	72 hours
Result:	Inhibits proliferation of multiple myeloma cell lines.

In Vivo

MLN120B (oral administration; 50 mg/kg; twice daily; 3 weeks) induces a reduction of shuIL-6R, marker of tumor growth, marker of tumor growth. It also leads to a rend toward prolonged survival in animals treated versus control ^[1] .
MLN120B (oral administration; 1-30 mg/kg; twice daily; 3 weeks) inhibits paw swelling in a dose-dependent manner and offers significant protection against arthritis-induced weight loss as well as cartilage and bone erosion. NF-κB activity in arthritic joints is also reduced after MLN120B administration ^[2] .

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

Animal Model:	Two-month-old female Lewis rats ^[2]
Dosage:	30 mg/kg, 10 mg/kg, 3 mg/kg, or 1 mg/kg
Administration:	Oral administration; twice daily; 3 weeks
Result:	Protected against bone and cartilage destruction in a rat model.

Animal Model:	SCID mice implanted with human fetal bone chips and then INA6 cells are directly injected into mice ^[1]
Dosage:	50 mg/kg
Administration:	Oral administration; twice daily; 3 weeks
Result:	Inhibited human multiple myeloma cell growth in vivo.

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 : ≥ 31 mg/mL ( 84.51 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7263 mL	13.6314 mL	27.2628 mL
5 mM	0.5453 mL	2.7263 mL	5.4526 mL
10 mM	0.2726 mL	1.3631 mL	2.7263 mL

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

In Vivo:

1.

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

Solubility: ≥ 2.5 mg/mL (6.82 mM); Clear solution
2.

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

Solubility: ≥ 2.08 mg/mL (5.67 mM); Clear solution
3.

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

Solubility: 2.08 mg/mL (5.67 mM); Suspended solution; Need ultrasonic

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