Powder: -20°C for 3 years | In solvent: -80°C for 2 years
JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | 6-8 weeks | $ 970.00
$ 776.00
|
|
50 mg | 6-8 weeks | $ 1,980.00
$ 1,584.00
|
|
100 mg | 6-8 weeks | $ 2,500.00
$ 2,000.00
|
Description | JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M. |
Targets&IC50 | EGFR L858R/T790M:0.26 nM |
In vitro | JBJ-04-125-02 demonstrates mutant selectivity by inhibiting mutant EGFR and downstream AKT and ERK1/2 phosphorylation.JBJ-04-125-02 (0-1000 nM; 72 hours; H1975 cells) treatment could inhibit cell proliferation of H1975 cells at low nanomolar concentrations. JBJ-04-125-02 treatment also inhibits cell proliferation in Ba/F3 cells stably transfected with EGFRL858R, EGFRL858R/T790M, or EGFRL858R/T790M/C797S mutations. The ability of JBJ-04-125-02 (0.01-10 μM) to inhibit EGFR phosphorylation using Ba/F3, H1975 and NIH-3T3 cells is examined. |
In vivo | JBJ-04-125-02 exhibits a moderate half-life of 3 hours and a high area under curve of 728,577 min?ng/mL (AUClast) following 3 mg/kg intravenous (i.v.) dose. A 20 mg/kg oral dose of JBJ-04-125-02 achieves an average maximal plasma concentration of 1.1 μmol/L with an oral bioavailability of 3%.JBJ-04-125-02 (50 mg/kg; oral gavage; once daily; for 15 weeks; EGFRL858R/T790M/C797S genetically engineered mice) treatment leads to marked tumor regressions within 4 weeks of treatment. |
Molecular Weight | 543.61 |
Formula | C29H26FN5O3S |
CAS No. | 2060610-53-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
JBJ-04-125-02 2060610-53-7 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells JAK JBJ0412502 JBJ 04 125 02 inhibitor inhibit