JBJ-02-112-05
JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFRL858R/T790M.
For research use only. We do not sell to patients.
- CAS No.: 2748162-29-8
- Formula: C27H20N4O2S
- Molecular Weight:464.54
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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All EGFR Isoforms
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Biological Activity
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EGFRL858R/T790M 15 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| BaF3 | IC50 |
0.9 μM
Compound: 5; JBJ-02-112-05
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Antiproliferative activity against mouse BaF3 cells stably transfected with EGFR L858R/T790M/C797S (unknown origin) assessed as inhibition of cell proliferation incubated for 72 hrs by MTS assay
Antiproliferative activity against mouse BaF3 cells stably transfected with EGFR L858R/T790M/C797S (unknown origin) assessed as inhibition of cell proliferation incubated for 72 hrs by MTS assay
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[PMID: 33243531] |
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[1].
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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[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[1]
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Dosage:100 mg/kg
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Administration:Oral gavage; once daily; for 3 days
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Result:Inhibited phosphorylation of EGFR and downstream signaling pathways.
Chemical Information
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CAS No. 2748162-29-8
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Molecular Weight 464.54
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Formula C27H20N4O2S
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SMILES
O=C(NC1=NC=CS1)C(N2C(C(C=C(C3=CC(C=CN4)=C4C=C3)C=C5)=C5C2)=O)C6=CC=CC=C6
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JBJ-02-112-05 Related Classifications
HY-135914 Related Classifications
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