IC50 Value: MLN120B (20 umol/L) induced up to 35% and 75% inhibition, assessed by MTT assay and [3H]thymidine uptakein multiple myeloma cell lines, respectively. NF-¦ÊB pathway blockers, such as MLN120B, are currently being explored for treatment of inflammatory diseases such as COPD and asthma[3]. in vitro: MLN120B inhibits both baseline and tumor necrosis factor-¦Á-induced nuclear factor-¦ÊB activation, associated with down-regulation of I¦ÊB¦Á and p65 nuclear factor-¦ÊB phosphorylation. MLN120B triggers 25% to 90% growth inhibition in a dose-dependent fashion in multiple myeloma cell lines and significantly augments tumor necrosis factor-¦Á-induced cytotoxicity in MM.1S cells. MLN120B augments growth inhibition triggered by doxorubicin and melphalan in both RPMI 8226 and IL-6-dependent INA6 cell lines. Neither IL-6 nor IGF-1 overcomes the growth-inhibitory effect of MLN120B. MLN120B inhibits constitutive IL-6 secretion by BMSCs by 70% to 80% without affecting viability. Importantly, MLN120B 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.MLN120B mediates anti-human multiple myeloma cell activity in vivo using a novel SCID-hu model, in which multiple myeloma cells grow in vivoin the context of the human bone marrow microenvironment. Eight SCID mice were implanted with human fetal bone chips (SCID-hu), into which human IL-6-dependent INA6 cells were directly injected. These mice were treated orally with either MLN120B (50 mg/kg) or vehicle control twice daily for 3 weeks[1]. Oral administration of ML120B inhibited paw swelling in a dose-dependent manner (median effective dosage 12 mg/kg twice daily) and offered significant protection against arthritis-induced weight loss as well as cartilage and bone erosion

June 21, 2017

prudect name : IC50 Value: MLN120B (20 umol/L) induced up to 35% and 75% inhibition, assessed by MTT assay and [3H]thymidine uptakein multiple myeloma cell lines, respectively. NF-¦ÊB pathway blockers, such as MLN120B, are currently being explored for treatment of inflammatory diseases such as COPD and asthma[3]. in vitro: MLN120B inhibits both baseline and tumor necrosis factor-¦Á-induced nuclear factor-¦ÊB activation, associated with down-regulation of I¦ÊB¦Á and p65 nuclear factor-¦ÊB phosphorylation. MLN120B triggers 25% to 90% growth inhibition in a dose-dependent fashion in multiple myeloma cell lines and significantly augments tumor necrosis factor-¦Á-induced cytotoxicity in MM.1S cells. MLN120B augments growth inhibition triggered by doxorubicin and melphalan in both RPMI 8226 and IL-6-dependent INA6 cell lines. Neither IL-6 nor IGF-1 overcomes the growth-inhibitory effect of MLN120B. MLN120B inhibits constitutive IL-6 secretion by BMSCs by 70% to 80% without affecting viability. Importantly, MLN120B 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.MLN120B mediates anti-human multiple myeloma cell activity in vivo using a novel SCID-hu model, in which multiple myeloma cells grow in vivoin the context of the human bone marrow microenvironment. Eight SCID mice were implanted with human fetal bone chips (SCID-hu), into which human IL-6-dependent INA6 cells were directly injected. These mice were treated orally with either MLN120B (50 mg/kg) or vehicle control twice daily for 3 weeks[1]. Oral administration of ML120B inhibited paw swelling in a dose-dependent manner (median effective dosage 12 mg/kg twice daily) and offered significant protection against arthritis-induced weight loss as well as cartilage and bone erosion
MLN120B

Synonyms: CAS NO: 783348-36-7Molecular Formula: C19H15ClN4O2Molecular Weight: 366.8Purity: 98% minSolubility: In DMSOStorage: -20°C


web site: www.medchemexpress.com

References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18534173