ONO-7475 是一种选择性的、有效的、具有口服活性的Axl/Mer抑制剂。它使 AXL 过表达的EGFR突变型 NSCLC 细胞对 EGFR-TKIs 敏感,抑制耐药细胞的产生和耐药性的维持。它与 Osimertinib 联合使用,具有用于 EGFR 突变非小细胞肺癌的潜力。
产品描述
ONO-7475 is an inhibitor with high specificity for anexelekto and MER tyrosine kinase
体外活性
ONO-7475 sensitized AXL-overexpressing?EGFR-mutant NSCLC cells to the EGFR-TKIs osimertinib and dacomitinib. In addition, ONO-7475 suppressed the emergence and maintenance of EGFR-TKI-tolerant cells[2].
体内活性
Mice fed a diet containing ONO-7475 exhibited significantly longer survival and, interestingly, blocked leukemia cell infiltration in the liver. In summary, ONO-7475 effectively kills acute myeloid leukemia cells?in vitro?and?in vivo?by mechanisms that involve disruption of diverse survival and proliferation pathways[1].
细胞实验
Cell Line:High AXL-expressing cell: PC-9,HCC4011,H1975, PC-9KGR cells. Low AXL-expressing cell: HCC827, HCC4006, and H3255 cells. Concentration:0.0001 μM; 0.001 μM; 0.01 μM; 0.1 μM; 1 μM. Incubation Time:72 hours[1].
Cas No.
1646839-59-9
分子式
C32H26N4O6
分子量
562.582
储存和溶解度
DMSO:100 mg/mL (177.76 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years