JBJ-09-063 TFA
Based on 1 Customer Validation
JBJ-09-063 TFA 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 TFA effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 TFA is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.64%
- Formel: C33H30F4N4O5S
- Molecular Weight:670.67
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
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) |
In Vitro
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.
In Vivo
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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Appearance Solid
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Molecular Weight 670.67
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Formel C33H30F4N4O5S
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Color White to off-white
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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.O=C(O)C(F)(F)F
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : ≥ 100 mg/mL (149.10 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. To C, et al. An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer. Nat Cancer. 2022 Apr;3(4):402-417. [Content Brief]
[2]. Gero TW, Scott DA, et al. Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC. Bioorg Med Chem Lett. 2022 Jul 15;68:128718. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4910 mL | 7.4552 mL | 14.9105 mL | 37.2762 mL |
| 5 mM | 0.2982 mL | 1.4910 mL | 2.9821 mL | 7.4552 mL | |
| 10 mM | 0.1491 mL | 0.7455 mL | 1.4910 mL | 3.7276 mL | |
| 15 mM | 0.0994 mL | 0.4970 mL | 0.9940 mL | 2.4851 mL | |
| 20 mM | 0.0746 mL | 0.3728 mL | 0.7455 mL | 1.8638 mL | |
| 25 mM | 0.0596 mL | 0.2982 mL | 0.5964 mL | 1.4910 mL | |
| 30 mM | 0.0497 mL | 0.2485 mL | 0.4970 mL | 1.2425 mL | |
| 40 mM | 0.0373 mL | 0.1864 mL | 0.3728 mL | 0.9319 mL | |
| 50 mM | 0.0298 mL | 0.1491 mL | 0.2982 mL | 0.7455 mL | |
| 60 mM | 0.0249 mL | 0.1243 mL | 0.2485 mL | 0.6213 mL | |
| 80 mM | 0.0186 mL | 0.0932 mL | 0.1864 mL | 0.4660 mL | |
| 100 mM | 0.0149 mL | 0.0746 mL | 0.1491 mL | 0.3728 mL |
JBJ-09-063 TFA Related Classifications
HY-147183A Related Classifications
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