JBJ-09-063
JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer.
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- CAS No.: 2820336-67-0
- Formule: C31H29FN4O3S
- Masse moléculaire:556.65
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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EGFR L858R 0.147 nM (IC50) |
EGFR L858R/T790M 0.063 nM (IC50) |
EGFR L858R/T790M/C797S 0.083 nM (IC50) |
EGFRLT/L747S 0.396 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
0.006 μM
Compound: 4; JBJ-09-063
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Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth in presence of cetuximab
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth in presence of cetuximab
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[PMID: 35378251] |
| BaF3 | IC50 |
0.05 μM
Compound: 4; JBJ-09-063
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Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth
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[PMID: 35378251] |
JBJ-09-063 is remarkably effective at inhibiting cell growth and leads to a significant increase in apoptosis, even though H3255GR cells are resistant to gefitinib as a single agent, as they contain an EGFR T790M mutation[1].
JBJ-09-063 is effective in H1975 cells exogenously expressing the osimertinib-resistant mutations[1].
JBJ-09-063 exhibits IC50s of 50 nM and 6 nM in Ba/F3 cell when use alone or combination with Cetuximab (HY-P9905)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[2]
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Dosage:3 mg/kg for i.v., 20 mg/kg for p.o.
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Administration:i.v. and p.o.; single dosage
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Result:Pharmacokinetic Parameters of JBJ-09-063 in mice[2].
Cl (mL/min/kg), i.v. T1/2 (h) Vss (L/kg) F (%) AUC 8h (ng·h/mL) 15.7 2.3 2.5 15 2398
Chemical Information
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CAS No. 2820336-67-0
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Masse moléculaire 556.65
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Formule C31H29FN4O3S
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SMILES
O=C(NC1=NC=CS1)C(C2=CC(F)=CC=C2O)N(CC3=C4C=C(C5=CC=C(C6CCN(C)CC6)C=C5)C=C3)C4=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvant et solubilité
DMSO : 120 mg/mL (215.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
Références
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7965 mL | 8.9823 mL | 17.9646 mL | 44.9115 mL |
| 5 mM | 0.3593 mL | 1.7965 mL | 3.5929 mL | 8.9823 mL | |
| 10 mM | 0.1796 mL | 0.8982 mL | 1.7965 mL | 4.4912 mL | |
| 15 mM | 0.1198 mL | 0.5988 mL | 1.1976 mL | 2.9941 mL | |
| 20 mM | 0.0898 mL | 0.4491 mL | 0.8982 mL | 2.2456 mL | |
| 25 mM | 0.0719 mL | 0.3593 mL | 0.7186 mL | 1.7965 mL | |
| 30 mM | 0.0599 mL | 0.2994 mL | 0.5988 mL | 1.4971 mL | |
| 40 mM | 0.0449 mL | 0.2246 mL | 0.4491 mL | 1.1228 mL | |
| 50 mM | 0.0359 mL | 0.1796 mL | 0.3593 mL | 0.8982 mL | |
| 60 mM | 0.0299 mL | 0.1497 mL | 0.2994 mL | 0.7485 mL | |
| 80 mM | 0.0225 mL | 0.1123 mL | 0.2246 mL | 0.5614 mL | |
| 100 mM | 0.0180 mL | 0.0898 mL | 0.1796 mL | 0.4491 mL |
JBJ-09-063 Related Classifications
HY-147183 Related Classifications
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