JBJ-09-063 hydrochloride
Based on 1 Customer Validation
JBJ-09-063 hydrochloride 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 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer.
For research use only. We do not sell to patients.
- Purity: 98.52%
- Formula: C31H30ClFN4O3S
- Molecular Weight:593.11
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Storage:
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All EGFR Isoforms
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Biological Activity
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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) |
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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Appearance Solid
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Molecular Weight 593.11
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Formula C31H30ClFN4O3S
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Color Off-white to light yellow
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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.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (168.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 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)
References
[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 | 1.6860 mL | 8.4301 mL | 16.8603 mL | 42.1507 mL |
| 5 mM | 0.3372 mL | 1.6860 mL | 3.3721 mL | 8.4301 mL | |
| 10 mM | 0.1686 mL | 0.8430 mL | 1.6860 mL | 4.2151 mL | |
| 15 mM | 0.1124 mL | 0.5620 mL | 1.1240 mL | 2.8100 mL | |
| 20 mM | 0.0843 mL | 0.4215 mL | 0.8430 mL | 2.1075 mL | |
| 25 mM | 0.0674 mL | 0.3372 mL | 0.6744 mL | 1.6860 mL | |
| 30 mM | 0.0562 mL | 0.2810 mL | 0.5620 mL | 1.4050 mL | |
| 40 mM | 0.0422 mL | 0.2108 mL | 0.4215 mL | 1.0538 mL | |
| 50 mM | 0.0337 mL | 0.1686 mL | 0.3372 mL | 0.8430 mL | |
| 60 mM | 0.0281 mL | 0.1405 mL | 0.2810 mL | 0.7025 mL | |
| 80 mM | 0.0211 mL | 0.1054 mL | 0.2108 mL | 0.5269 mL | |
| 100 mM | 0.0169 mL | 0.0843 mL | 0.1686 mL | 0.4215 mL |
JBJ-09-063 hydrochloride Related Classifications
HY-147183B Related Classifications
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