ASP 3026 是一种选择性的，具有口服活性的间变性淋巴瘤激酶抑制剂，可诱导肿瘤细胞凋亡，可研究非小细胞肺癌。

ASP3026 has been used in trials studying the treatment of Solid Tumor, B-Cell Lymphoma, Advanced Malignancies, Positive for Anaplastic Lymphoma Kinase, and Positive for Proto-Oncogene Tyrosine-Protein Kinase ROS.

以每天两次口服给药ASP3026的方式处理荷有皮下NCI-H2228肿瘤异种移植物的小鼠14天,诱导剂量依赖性的抗肿瘤作用,从1 mg/kg开始,在10,30和100 mg/kg强烈消退.

ASP3026抑制内源性表达EML4-ALK变体3的人NSCLC肿瘤细胞系NCI-H2228的生长,IC50值为64.8 nM。ASP3026在酪氨酸激酶中比PF02341066显示更强的选择性抑制ALK活性。

Recombinant truncated FLAG-tagged mTOR expressed in HEK 293 cells is used in biochemical assays, together with a biotinylated p70S6K peptide substrate. Streptavidin donor and protein A acceptor beads are used to assemble the capture complex for generation of the assay signal. The activity of the lipid kinases, PI3K alpha, beta, delta, and gamma are measured using recombinant proteins and the lipid PIP2 as substrate. Assays for ATM and DNA-PK activity are performed. The mTOR cellular activity is measured in MDAMB468 cells, using an Acumen laser scanning cytometer to analyze the levels of phosphorylation of S6 (Ser235/236) and AKT (Ser473)[1].

1097917-15-1

C29H40N8O3S

580.74

ASP 3026

DMSO:11.6 mg/mL (20 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years