JANEX-1

Description: JANEX-1 (aslo known as WHI-P131) is a novel, potent and selective inhibitor of the Janus kinase 3 (JAK3) that selectively inhibits JAK3 with an IC50 of 78 uM and does not inhibit JAK1 and JAK2. It triggers apoptosis in human acute lymphoblastic leukemia (ALL) cells. Following i.v. administration, the terminal elimination half-life of WHI-P131 was 73.2 min in rats, 103.4 min in mice, and 45.0 min in monkeys. The i.v. administered WHI-P131 showed a very wide tissue distribution in mice. Following i.p. administration, WHI-P131 was rapidly absorbed in both rats and mice, and the time to reach the maximum plasma concentration (tmax) was 24.8 min in rats and 10.0 min in mice.

References: Clin Cancer Res. 1999 Oct; 5(10):2954-62; Exp Mol Med. 2013 May 17; 45:e23