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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
EGFRL858R/T790M 15 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 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 Vitro
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. Further protocols information, click here.
In Vivo
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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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