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Medchemexpress LLC Jh-viii-157-02 | 1639422-97-1 | 98.98% | 465.55 | 25 MG

Supplier: Medchemexpress LLC 25MGHY112140
JH-VIII-157-02 is a structural analogue of alectinib, functioning as an ALK inhibitor. It exhibits an IC50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells. It also potently inhibits various EML4-ALK mutants and shows selectivity at other kinases.
- Inhibits EML4-ALK G1202R (IC50, 2 nM).
- Potent inhibition of EML4-ALKwt, EAC1156Y, EAF1174L, EAS1206Y (IC50, 2 nM), EAG1269A (IC50, 3 nM), EAL1196M (IC50, 58 nM), EA1151Tins (IC50, 107 nM), and EAL1152R (IC50, 196 nM).
- Selective inhibition of other kinases including IRAK1, CLK4, RET, RET V804L, RET V804M and IRAK 4.
- Inhibits growth in cancer cell lines like H3122 and DFCI76 (L1152R) with EC50s of 5 and 19 nM.
- Good oral bioavailability at 10 mg/kg in mice.
- Penetrates the CNS of mice.
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