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编 号：F741751
分子式：C27H20N4O2S
分子量：464.54
分子式：C27H20N4O2S
分子量：464.54
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CAS No: 2748162-29-8
产品详情
生物活性：
JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFRL858R/T790M.
体内研究：
JBJ-02-112-05 (100 mg/kg; oral gavage; once daily; for 3 days; EGFRL858R/T790M/C797S genetically engineered mice) treatment inhibits phosphorylation of EGFR and downstream signaling pathways.JBJ-02-112-05 exhibits a moderate half-life of 3 hours and a Cmax of 13.7 μM following 3 mg/kg intravenous (i.v.) dose. A 5 mg/kg oral dose of JBJ-02-112-05 achieves a half-life of 16.4 hours and a CCmax of 1.31 μM.Animal Model:EGFRL858R/T790M/C797S genetically engineered mice
Dosage:100 mg/kg
Administration:Oral gavage; once daily; for 3 days
Result:Inhibited phosphorylation of EGFR and downstream signaling pathways.
体外研究：
In Ba/F3 cells, JBJ-02-112-05 inhibits the activities of wildtype EGFR, EGFRL858R, EGFRL858R/T790M and EGFRL858R/T790M/C797S with IC50 values of 9.29 μM; 8.35 μM; 8.53 μM and 2.13 μM, respectively.JBJ-02-112-05 demonstrates mutant selectivity by inhibiting mutant EGFR and downstream AKT and ERK1/2 phosphorylation in Ba/F3 cells stably transfected with EGFRL858R, EGFRL858R/T790M, EGFRL858R/T790M/C797S mutations.
JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFRL858R/T790M.
体内研究：
JBJ-02-112-05 (100 mg/kg; oral gavage; once daily; for 3 days; EGFRL858R/T790M/C797S genetically engineered mice) treatment inhibits phosphorylation of EGFR and downstream signaling pathways.JBJ-02-112-05 exhibits a moderate half-life of 3 hours and a Cmax of 13.7 μM following 3 mg/kg intravenous (i.v.) dose. A 5 mg/kg oral dose of JBJ-02-112-05 achieves a half-life of 16.4 hours and a CCmax of 1.31 μM.Animal Model:EGFRL858R/T790M/C797S genetically engineered mice
Dosage:100 mg/kg
Administration:Oral gavage; once daily; for 3 days
Result:Inhibited phosphorylation of EGFR and downstream signaling pathways.
体外研究：
In Ba/F3 cells, JBJ-02-112-05 inhibits the activities of wildtype EGFR, EGFRL858R, EGFRL858R/T790M and EGFRL858R/T790M/C797S with IC50 values of 9.29 μM; 8.35 μM; 8.53 μM and 2.13 μM, respectively.JBJ-02-112-05 demonstrates mutant selectivity by inhibiting mutant EGFR and downstream AKT and ERK1/2 phosphorylation in Ba/F3 cells stably transfected with EGFRL858R, EGFRL858R/T790M, EGFRL858R/T790M/C797S mutations.
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