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Catalog: | HY-15473A |
Brand: | MCE |
CAS: | 1782573-78-7 |
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 |
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. |
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. |
Solid
Room temperature in continental US; may vary elsewhere.
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
DMSO : 16.67 mg/mL ( 37.91 mM ; ultrasonic and warming and adjust pH to 8 with NaOH and heat to 80°C)
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 |
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