JBJ-04-125-02
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. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities.
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- CAS. Nr.: 2060610-53-7
- Formel: C29H26FN5O3S
- Molecular Weight:543.61
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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EGFR (L858R/T790M) 0.26 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1975 | IC50 |
1.25 μM
Compound: JBJ-04-125-02
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Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs in presence of osimertinib by CellTiter-Glo luminescent assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs in presence of osimertinib by CellTiter-Glo luminescent assay
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[PMID: 38142512] |
| NCI-H1975 | IC50 |
3.66 μM
Compound: JBJ-04-125-02
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Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 38142512] |
JBJ-04-125-02 (0-1000 nM; 72 hours; H1975 cells) treatment could inhibit cell proliferation of H1975 cells at low nanomolar concentrations[1].
JBJ-04-125-02 treatment also inhibits cell proliferation in Ba/F3 cells stably transfected with EGFRL858R, EGFRL858R/T790M, or EGFRL858R/T790M/C797S mutations[1].
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. JBJ-04-125-02 demonstrates mutant selectivity by inhibiting mutant EGFR and downstream AKT and ERK1/2 phosphorylation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H1975 cells
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Concentration:0 nM, 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM
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Incubation Time:72 hours
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Result:Inhibited cell proliferation of H1975 cells at low nanomolar concentrations.
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%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:EGFRL858R/T790M/C797S genetically engineered mice (GEM)[1]
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Dosage:50 mg/kg
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Administration:Oral gavage; once daily; for 15 weeks
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Result:Led to marked tumor regressions within 4 weeks of treatment.
Chemical Information
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CAS. Nr. 2060610-53-7
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Molecular Weight 543.61
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Formel C29H26FN5O3S
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SMILES
O=C(NC1=NC=CS1)[C@@H](C2=CC(F)=CC=C2O)N(CC3=C4C=C(C5=CC=C(N6CCNCC6)C=C5)C=C3)C4=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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