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CAS No. : 1639422-97-1
MCE 国际站:JH-VIII-157-02
产品活性:JH-VIII-157-02 是 alectinib 的结构类似物,为 ALK 抑制剂,对棘皮动物微管相关蛋白样 4 (EML4)-ALK G1202R 的 IC50 值为 2 nM。
研究领域:Protein Tyrosine Kinase/RTK
作用靶点:Anaplastic lymphoma kinase (ALK)
In Vitro: JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells. JH-VIII-157-02 also potently inhibits EML4-ALKwt (Eawt), EAC1156Y, EAF1174L, EAS1206Y (IC50, 2 nM), EAG1269A (IC50, 3 nM), EAL1196M (IC50, 58 nM), EA1151Tins (IC50, 107 nM), and EAL1152R (IC50, 196 nM). Moreover, JH-VIII-157-02 has selectivity at other kinases, including IRAK1, CLK4, RET, RET V804L, RET V804M and IRAK 4, and the IC50s are 14 nM, 14 nM, 3 nM, 13 nM, 12 nM, and 465 nM respectively. JH-VIII-157-02 exhibits inhibitory growth of cancer cell lines, such as H3122, DFCI76 (L1152R] with EC50s of 5, 19 nM, respectively.
In Vivo: JH-VIII-157-02 exhibits good oral bioavailability following an oral dose of 10 mg/kg in mice. JH-VIII-157-02 also penetrates the CNS of mice.
相关产品:Bioactive Compound Library Plus | ALK/ROS1-IN-1 | Ceritinib | KRCA-0008 | Iruplinalkib | ALK-IN-22 | NVP-TAE 684 | TL13-110 | Brigatinib-13C6 | Alectinib | Zotizalkib | M4K2234 | Con B-1 | Ficonalkib | Entrectinib | 2-Keto Crizotinib | ALK inhibitor 1 | ALK-IN-6 | GSK1838705A | EML4-ALK kinase inhibitor 1 | F-1 | ALK-IN-1 | MS4077 | ALK kinase inhibitor-1 | CJ-2360 | Envonalkib | MS4078 | ALK-IN-5 | X-376
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