| 生化机理 |
Description: IC50 Value: 5uM (inhibit U251, SF188, T98G cell growth in monolayer after 72h) VAL-083 surpasses temozolomide (TMZ) activity and inhibits cancer stem cells (CSCs) providing a new potential treatment option for glioblastoma multiforme (GBM). VAL-083 inhibited U251 and SF188 cell growth in monolayer better than TMZ and caused apoptosis [1]. in vitro: VAL-083 inhibited U251 and SF188 cell growth in monolayer and as neurospheres better than TMZ and caused apoptosis after 72 hr. In the colony formation assay, VAL-083 (5 uM) suppressed SF188 growth by about 95%. T98G cells are classically TMZ-resistant and express MGMT, but VAL-083 inhibited their growth in monolayer after 72 hr in a dose-dependent manner (IC50, 5 uM). VAL-083 also inhibited the growth of CSCs (BT74, GBM4, and GBM8) by 80-100% in neurosphere self-renewal assays. Conversely, there was minimal effect on normal human neural stem cells [1]. in vivo: N/A Clinical trial: Safety Study of VAL-083 in Pat |
