Powder: -20°C for 3 years | In solvent: -80°C for 1 year
JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active inhibitor of EGFR with an IC 50 of 15 nM for EGFR L858R/T790M [1].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 10-14 weeks | $ 1,520.00 | |
50 mg | 10-14 weeks | $ 1,980.00 | |
100 mg | 10-14 weeks | $ 2,500.00 |
Description | JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active inhibitor of EGFR with an IC 50 of 15 nM for EGFR L858R/T790M [1]. |
Targets&IC50 | EGFRL858R/T790M:15 nM |
In vitro | In Ba/F3 cells, JBJ-02-112-05 inhibits the activities of wildtype EGFR, EGFR L858R, EGFR L858R/T790M and EGFR L858R/T790M/C797S with IC 50 values of 9.29 μM; 8.35 μM; 8.53 μM and 2.13 μM, respectively [1]. JBJ-02-112-05 shows mutant selectivity through inhibiting mutant EGFR and downstream AKT and ERK1/2 phosphorylation in Ba/F3 cells stably transfected with EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S mutations [1]. |
In vivo | Treatment with JBJ-02-112-05 (100 mg/kg; oral gavage; once daily; for 3 days; EGFR L858R/T790M/C797S genetically engineered mice) can inhibit phosphorylation of EGFR and downstream signaling pathways [1]. 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 C Cmax of 1.31 μM [1]. Animal Model: EGFR L858R/T790M/C797S genetically engineered mice [1] Dosage: 100 mg/kg Administration: Oral gavage; once daily; for 3 days Result: Inhibited phosphorylation of EGFR and downstream signaling pathways. |
Molecular Weight | 464.54 |
Formula | C27H20N4O2S |
CAS No. | 2748162-29-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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JBJ-02-112-05 2748162-29-8 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells JAK JBJ0211205 JBJ 02 112 05 inhibitor inhibit