Osimertinib-d6
Based on 1 Customer Validation
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
For research use only. We do not sell to patients.
- Purity: 99.64%
- CAS No.: 1638281-44-3
- Formula: C28H27D6N7O2
- Molecular Weight:505.64
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Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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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
All EGFR Isoforms
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Biological Activity
Osimertinib (AZD9291) (0-10 μM; 72 hours) dramatically inhibits cell proliferation with IC50s of 41, 26, 41, and 31 nM, respectively[2].
Osimertinib (0-10 μM; 72 hours) inhibits cell proliferation (Ba/F3 cells harboring a T790M mutation, exon 19del+T790M, or L858R+T790M) with IC50s of 6, 7, and 74 nM, respectively[2].
Osimertinib (0-10 μM; 72 hours) inhibits Ba/F3 cells harboring EGFR exon 20 insertion mutations (IC50 ranging from 16-701 nM for A763_Y764insFQEA (FQEA), Y764_V765insHH (HH), A767_V769dupASV (ASV), and D770_N771insNPG (NPG) cells) [2].
Osimertinib shows high levels of phenotype potency in both sensitizing-mutant (mean IC50 of 8 nM in PC-9) and T790M (mean IC50 of 11 and 40 nM in H1975 and PC-9VanR respectively) EGFR cell lines. Osimertinib has much less activity towards wild-type EGFR (mean IC50 of 650 and 461 nM in Calu3 and H2073 respectively)[1].
Osimertinib (0.1 μM; 48 hours) induces apoptosis in Ba/F3 cells (apoptosis rate of 40.9% and 90% in EGFR exon 19del+T790M, EGFR L858R+T790M respectively) [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC-9, H3255, PC-9ER, and H1975 cells
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Concentration:0.0001, 0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:72 hours
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Result:Dramatically inhibited cell proliferation (IC50=41,26, 41, 31 nM, respectively)
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Cell Line:Ba/F3 cells (harboring a T790M mutation, exon 19del+T790M, or L858R+T790M)
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Concentration:0.0001, 0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:72 hours
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Result:Inhibited cell proliferation (IC50 = 6, 7, 74 nM, respectively)
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Cell Line:Ba/F3 cells (harboring EGFR exon 20 insertion mutations)
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Concentration:0.0001, 0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:72 hours
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Result:Inhibited cell proliferation (IC50 = 16, 701, 230, 38 nM, respectively)
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Cell Line:Ba/F3 cells(harboring EGFR exon 19del+T790M or EGFR L858R+T790M)
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Concentration:0.1 μM
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Incubation Time:48 hours
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Result:Inducted apoptosis with the rate of 40.9% and 90% in EGFR T790M positive mutations cells respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1]
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Dosage:0.1-10 mg/kg (PC-9 xenograft models); 0.5- 25 mg/kg (H1975 xenograft models)
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Administration:p.o.; daily for 14 day
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Result:Induced significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 1638281-44-3
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Unlabeled Cas 1421373-65-0
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Appearance Solid
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Molecular Weight 505.64
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Formula C28H27D6N7O2
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Color White to light yellow
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SMILES
C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C([2H])([2H])[2H])C([2H])([2H])[2H])C)=O
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Synonyms
AZD-9291-d6; Mereletinib-d6
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : 125 mg/mL (247.21 mM; ultrasonic and warming and heat to 60°C; 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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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 (282 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61. [Content Brief]
[2]. [2]Hirano T, et al. Pharmacological and Structural Characterizations of Naquotinib, a Novel Third-Generation EGFR Tyrosine Kinase Inhibitor, in EGFR-Mutated Non-Small Cell Lung Cancer. Mol Cancer Ther. 2018 Apr;17(4):740-750. [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 (protect from light, stored under nitrogen). 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 | 1.9777 mL | 9.8885 mL | 19.7769 mL | 49.4423 mL |
| 5 mM | 0.3955 mL | 1.9777 mL | 3.9554 mL | 9.8885 mL | |
| 10 mM | 0.1978 mL | 0.9888 mL | 1.9777 mL | 4.9442 mL | |
| 15 mM | 0.1318 mL | 0.6592 mL | 1.3185 mL | 3.2962 mL | |
| 20 mM | 0.0989 mL | 0.4944 mL | 0.9888 mL | 2.4721 mL | |
| 25 mM | 0.0791 mL | 0.3955 mL | 0.7911 mL | 1.9777 mL | |
| 30 mM | 0.0659 mL | 0.3296 mL | 0.6592 mL | 1.6481 mL | |
| 40 mM | 0.0494 mL | 0.2472 mL | 0.4944 mL | 1.2361 mL | |
| 50 mM | 0.0396 mL | 0.1978 mL | 0.3955 mL | 0.9888 mL | |
| 60 mM | 0.0330 mL | 0.1648 mL | 0.3296 mL | 0.8240 mL | |
| 80 mM | 0.0247 mL | 0.1236 mL | 0.2472 mL | 0.6180 mL | |
| 100 mM | 0.0198 mL | 0.0989 mL | 0.1978 mL | 0.4944 mL |
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