JH-VIII-157-02 is a structural analogue of alectinib, functioning as an ALK inhibitor. It exhibits an IC50 of 2 nM for EML4-ALK G1202R in cells and potently inhibits various other EML4-ALK mutants and wild type (e.g., EML4-ALKwt, EAC1156Y, EAF1174L, EAS1206Y with IC50s of 2-196 nM). It shows selectivity at other kinases like IRAK1, CLK4, RET, and IRAK 4. JH-VIII-157-02 demonstrates inhibitory growth against cancer cell lines like H3122 and DFCI76 (EC50s of 5 nM and 19 nM). It also has good oral bioavailability and penetrates the CNS in mice.
- Structural analogue of alectinib
- Acts as an ALK inhibitor
- Shows potent inhibition of EML4-ALK G1202R mutant (IC50 of 2 nM)
- Potently inhibits other EML4-ALK mutants and wild type
- Exhibits selectivity at several other kinases
- Inhibits growth of cancer cell lines
- Good oral bioavailability in mice
- Penetrates the CNS of mice