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].
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
25 mg | 約10-14 週間 | ¥ 349,000 |
50 mg | 約10-14 週間 | ¥ 454,500 |
100 mg | 約10-14 週間 | ¥ 574,000 |
説明 | 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]. |
ターゲット&IC50 | EGFR (L858R/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 | Administering JBJ-02-112-05 (100 mg/kg; oral gavage; once daily for 3 days) to EGFR L858R/T790M/C797S genetically engineered mice effectively inhibits the phosphorylation of EGFR and downstream signaling pathways [1]. This compound has a moderate half-life of 3 hours and reaches a peak concentration (Cmax) of 13.7 μM after an intravenous (i.v.) dose of 3 mg/kg. Furthermore, a 5 mg/kg oral dosage achieves a prolonged half-life of 16.4 hours with a Cmax of 1.31 μM [1]. |
分子量 | 464.54 |
分子式 | C27H20N4O2S |
CAS No. | 2748162-29-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. 詳細
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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 inhibitor inhibit