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Osimertinib (AZD-9291) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR, respectively. In vivo, AZD9291 shows significantly more potent inhibition of proliferation in mutant EGFR cell lines when compared with wild-type. AZD9291(5mg/kg p.o.) causes profound regression of tumors across EGFRm+ (PC9) and EGFRm+/T790M (H1975) tumor models with profound inhibition of EGFR phosphorylation and key downstream signaling pathways such as AKT and ERK.
J Pharm Anal. 2024 Jul 18.
Strategy for Cysteine-Targeting Covalent Inhibitors Screening using In-house Database based LC-MS/MS and Drug Repurposing
AZD9291 (Osimertinib) purchased from AbMole
Mol Cancer Ther. 2022 Jul 5;21(7):1060-1066.
HJM-561, a Potent, Selective, and Orally Bioavailable EGFR PROTAC that Overcomes Osimertinib-Resistant EGFR Triple Mutations
AZD9291 (Osimertinib) purchased from AbMole
Bioengineered. 2022 Jan;13(1):331-344.
AZD3759 enhances radiation effects in non-small-cell lung cancer by a synergistic blockade of epidermal growth factor receptor and Janus kinase-1
AZD9291 (Osimertinib) purchased from AbMole
Chem Res Toxicol. 2021 Nov 15;34(11):2309-2318.
Quantification of Osimertinib and Metabolite–Protein Modification Reveals Its High Potency and Long Duration of Effects on Target Organs
AZD9291 (Osimertinib) purchased from AbMole
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AZD3759 inhibits glioma through the blockade of the epidermal growth factor receptor and Janus kinase pathways
AZD9291 (Osimertinib) purchased from AbMole
Clin Cancer Res. 2018 Nov 15;24(22):5658-5672.
Increased Synthesis of MCL-1 Protein Underlies Initial Survival of EGFR-Mutant Lung Cancer to EGFR Inhibitors and Provides a Novel Drug Target.
AZD9291 (Osimertinib) purchased from AbMole
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Source | Clinical Cancer Research (2018 Nov). Figure 1. osimertinib (Abmole Bioscience) |
| Method | Western Blot | |
| Cell Lines | EGFR mutant NSCLC cell lines | |
| Concentrations | 50 nM | |
| Incubation Time | 72 h | |
| Results | In both sets of DTCs, other than BCL-2 in the PC9 osimertinib-DTCs, other anti-apoptotic BCL-2 family members were not upregulated, and, with the exception of NOXA in the HCC827 gefitinib-DTCs, expression of the key pro-apoptotic BCL-2 family members BIM and NOXA was not markedly diminished. |
 |
Source | Nat Med (2015). Figure 1. AZD9291 |
| Method | digital PCR (ddPCR) assay | |
| Cell Lines | Ba/F3 cells | |
| Concentrations | 1.0 μM | |
| Incubation Time | 72 h | |
| Results | Although a more comprehensive analysis of plasma and biopsy tissue collected after resistance develops will be needed to provide greater clarity on C797S mutation incidence, the emergence of this mutation in a marked proportion of AZD9291-resistant patients suggests that development of targeted therapies with the ability to overcome the C797S mutation is warranted. |
| Cell Experiment | |
|---|---|
| Cell lines | PC-9, H1975, LOVO, H1650 and H3255 lines |
| Preparation method | In vitro EGFR phosphorylation assays Cells were treated for 2 h with a dose-response of each drug. Wild-type cells were stimulated for 10 minutes with 25 ng/ml of EGF before lysis. Level of EGFR phosphorylation was quantified in cell extracts using a modified R&D Systems DuoSet Human phospho-EGFR ELISA (36). |
| Concentrations | 0-1000nM |
| Incubation time | 2h |
| Animal Experiment | |
|---|---|
| Animal models | PC-9 and H1975 cells subcutaneous xenograft models |
| Formulation | not mentioned |
| Dosages | 5 mg/kg/day QD |
| Administration | oral |
| Molecular Weight | 499.61 |
| Formula | C28H33N7O2 |
| CAS Number | 1421373-65-0 |
| Solubility (25°C) | DMSO 90 mg/mL (Need warming and ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Xiao-E Yan, et al. Structural Basis of AZD9291 Selectivity for EGFR T790M
[4] Pasi A Jnne, et al. AZD9291 in EGFR inhibitor-resistant non-small-cell lung cancer
| Related EGFR/HER2 Products |
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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. |
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