AP26113 是一种高效的、选择性的 ALK 激酶抑制剂，摘自专利 US20140066406 A1。

AP26113 is a potent ALK inhibitor with IC50 of 0.62 nM in a cell-free assay, demonstrated ability overcome Crizotinib resistance mediated by a L1196M mutation. Phase 2.

在HCC827(EGFR-DEL)或HCC827(EGFR-DEL/T790M)移植瘤小鼠模型中,AP26113（25 mg/kg）,能够抑制肿瘤细胞生长.在Karpas-299移植瘤小鼠模型中,AP26113（<50 mg/kg）抑制p-ALK.在Karpas-299移植瘤小鼠模型和 H3122 移植瘤小鼠模型中,AP26113（<50 mg/kg）抑制肿瘤生长.

在SU-DHL-1（GI50=9 nM）, H3122 （GI50=4 nM）和 Ba/F3-EML4-ALK v1（1 gI50=3 nM）细胞系中,抑制生长细胞生长。在表达EGFR-DEL(HCC827)的NSCLC细胞系中（IC50=62 nM）,AP26113作用于抑制EGFR 磷酸化,抑制细胞生长。

Three-day cell viability assays are carried out by plating 2,000, 1,500 and 2,000 cells per well of Ba/F3, PC9 or MGH121, respectively, into black transparent-bottom 96-well plates. On the same day for Ba/F3 cells and the following day for PC9 and MGH121 cells, the cells are treated with each TKI across a 10-dose range from 0.3 nM to 10 μM. After 72 h of drug treatment, cell viability is measured using the CellTiter-Glo assay. (Only for Reference)

1197958-12-5

C26H34ClN6O2P

529.02

Brigatinib;AP26113;AP26113-analog

Ethanol:98 mg/mL (185.3 mM)
DMSO:42 mg/mL (79.4 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years