DS-1205b free base 是有效的AXL激酶选择性抑制剂，IC50为 1.3 nM。它对MER，MET和TRKA也有抑制作用，IC50分别为 63、104 和 407 nM。 它可以抑制细胞迁移和肿瘤生长。

DS-1205 is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205 also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205 can inhibit cell migration in vitro and tumor growth in vivo[1].

DS-1205 (0.3-33 μM; 2-24 h) inhibits hGAS6-induced migration in NIH3T3-AXL cells (EC50=2.7 nM)[1]. DS-1205 (1-10000 μM; 2-24 h) significantly inhibits the phosphorylation of AXL in NIH3T3-AXL cells. DS-1205 decreases NIH3T3 cell proliferation but not obviously inhibits growth (GI50>10,000 nM)[1].

DS-1205 (3.1-50 mg/kg; p.o. bid for 5 d) exhibits pAXL inhibition mediated antitumor effects in mice[1].

1855860-24-0

C14H16N6O

284.32

DMSO:45 mg/mL (61.16 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years