All AbMole products are for research use only, cannot be used for human consumption.
-chemical-structure.gif)
Osimertinib mesylate (AZD-9291 mesylate) is a third-generation EGFR inhibitor, shows similar potency to early generation tyrosine kinase inhibitor (TKIs) in inhibiting EGFR phosphorylation in EGFR cells harboring sensitising EGFR mutants including PC-9 (ex19del), H3255 (L858R) and H1650 (ex19del), with mean IC50 values ranging from 13 to 54 nM for Osimertinib. Osimertinib (AZD-9291) also potently inhibits phosphorylation of EGFR in T790M mutant cell lines (H1975 (L858R/T790M), PC-9VanR (ex19del/T790M), with mean IC50 potency less than 15 nM.
 |
Source | Mol Pharm (2016). Figure 2.AZD-9291 |
| Method | immunoblotting | |
| Cell Lines | cancer cell lines | |
| Concentrations | 0.1 - 1 μM | |
| Incubation Time | 72 h | |
| Results | Cells were maintained in the absence or presence of increasing concentrations (0.1 - 1 μM) of osimertinib for 72 h, harvested and processed for immunoblotting as described in Materials and methods. |
 |
Source | Mol Pharm (2016). Figure 1.AZD-9291 |
| Method | flow cytometry | |
| Cell Lines | MDR19-HEK293 cells | |
| Concentrations | 10 μM | |
| Incubation Time | 24 h | |
| Results | Osimertinib (10 μM) significantly increased the accumulation of fluorescent calcein, an established substrate of ABCB145 in ABCB1-overexpressing KB-V-1 cells and ABCB1-transfected MDR19-HEK293 cells to the same extent as tariquidar, a known inhibitor of ABCB1 |
| Cell Experiment | |
|---|---|
| Cell lines | PC-9 cells |
| Preparation method | Media changes are carried out every 2-3 days and resistant clones allowed to grow to 80% confluency prior to the cells being trypsinised and reseeded at the original seeding density in media containing twice the concentration of EGFR inhibitor. Dose escalations are continued until a final concentration of 1.5 μM Gefitinib, 1.5 μM Afatinib, 1.5 μM WZ4002 or 160 nM AZD-9291 are achieved. |
| Concentrations | 160 nM |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | Mice |
| Formulation | 1% Polysorbate 80 |
| Dosages | 7.5 mg/kg and 5 mg/kg |
| Administration | oral |
| Molecular Weight | 595.71 |
| Formula | C29H37N7O5S |
| CAS Number | 1421373-66-1 |
| Solubility (25°C) | DMSO 9 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related EGFR/HER2 Products |
|---|
| Sevabertinib
Sevabertinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor with antitumor activity. |
| BPIQ-I
BPIQ-I (PD 159121) is a potent and ATP-competitive EGFR tyrosine kinase inhibitor.. |
| HKI-357
HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. |
| SJF-1528
SJF-1528 is a potent EGFR PROTAC degrader with DC50 values of 39.2 nM and 736.2 nM for wild-type EGFR in OVCAR8 cells and Exon 20 Ins mutated EGFR in HeLa cells. |
| CH7233163
CH7233163 is a noncovalent ATP-competitive inhibitor for EGFR-Del19/T790M/C797S. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
