Description |
ERK-IN-7 (Example 10), an analogue of SHR2415 (HY-151367), is a potent ERK inhibitor with IC50 of 5 nM and 7 nM against ERK1 and ERK2, respectively[1].
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Related Catalog |
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Target |
ERK1:5 nM (IC50)
ERK2:7 nM (IC50)
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In Vitro |
ERK-IN-7 (Example 10; 24 h) 抑制 Colo205 增殖,IC50 为 62 nM[1]。 Cell Proliferation Assay[1] Cell Line: Colo205 Concentration: Incubation Time: 24 h Result: Inhibited proliferation with an IC50 of 62 nM.
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In Vivo |
ERK-IN-7 (Example 10; 2 mg/kg; i.g.) 具有良好的药代动力学结果[1] Animal Model: C57 mice[1] Dosage: 2 mg/kg Administration: Intragastric administration (Pharmacokinetic Analysis) Result: Pharmacokinetic parameters[1] Cmax (ng/mL) AUC (ng⋅h/mL) T1/2 (h) MRT (h) CLz/F (mL/min/kg) Vz/F (mL/kg) ERK-IN-7 (Example 10) 1023 3441 3.66 3.47 9.69 3067
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References |
[1]. Xin Li, et al. Pyrroloheterocyclic derivative, preparation method therefor, and application thereof in medicine. Patent WO2020200069A1.
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