[CAS NO. 1782573-78-7] MLN120Bdihydrochloride

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PRODUCTS SPECIFICATIONS [1782573-78-7]

Catalog

HY-15473A

Brand

MCE

CAS

1782573-78-7

DESCRIPTION [1782573-78-7]

Overview

MDL	-
Molecular Weight	439.72
Molecular Formula	C19H17Cl3N4O2
SMILES	ClC1=C(C(NC(C2=CC=CN=C2C)=O)=C3C(C4=C(N3)C=NC=C4)=C1)OC.Cl.Cl

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

18 Publications Citing Use of MCE

Summary

MLN120B dihydrochloride (ML120B dihydrochloride) 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] .

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:	5 μM; 10 μM; 20 μM
Incubation Time:	90 mintues
Result:	Inhibited p-IκB and p-P65 expression in a dose-dependent manner.

Cell Viability Assay ^[1]

Cell Line:	Myeloma cell lines: MM.1S, MM.1R, RPMI 8226, RPMI-LR5, RPMI-Dox40, U266, and INA6 cells
Concentration:	0-40 μM
Incubation Time:	72 hours
Result:	Inhibited 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; 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 ^[3] .

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

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.

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.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 16.67 mg/mL ( 37.91 mM ; ultrasonic and warming and adjust pH to 8 with NaOH and heat to 80°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2742 mL	11.3709 mL	22.7417 mL
5 mM	0.4548 mL	2.2742 mL	4.5483 mL
10 mM	0.2274 mL	1.1371 mL	2.2742 mL

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