Osimertinib dimesylate
- Product Name
- Osimertinib dimesylate
- CAS No.
- 2070014-82-1
- Chemical Name
- Osimertinib dimesylate
- Synonyms
- Osimertinib dimesylate
- CBNumber
- CB05419799
- Molecular Formula
- C29H37N7O5S
- Formula Weight
- 595.72
- MOL File
- 2070014-82-1.mol
Osimertinib dimesylate Property
- storage temp.
- Store at -20°C
- solubility
- DMSO: 0.4 mg/mL (0.58 mM and warming)
- form
- Solid
- color
- Light yellow to yellow
N-Bromosuccinimide Price
- Product number
- CS-3405
- Product name
- Osimertinibdimesylate
- Purity
- 99.96%
- Packaging
- 5mg
- Price
- $60
- Updated
- 2021/12/16
- Product number
- CS-3405
- Product name
- Osimertinibdimesylate
- Purity
- 99.96%
- Packaging
- 10mg
- Price
- $70
- Updated
- 2021/12/16
- Product number
- CS-3405
- Product name
- Osimertinibdimesylate
- Purity
- 99.96%
- Packaging
- 50mg
- Price
- $100
- Updated
- 2021/12/16
- Product number
- CS-3405
- Product name
- Osimertinibdimesylate
- Purity
- 99.96%
- Packaging
- 100mg
- Price
- $120
- Updated
- 2021/12/16
- Product number
- CS-3405
- Product name
- Osimertinibdimesylate
- Purity
- 99.96%
- Packaging
- 200mg
- Price
- $140
- Updated
- 2021/12/16
Osimertinib dimesylate Chemical Properties,Usage,Production
Description
Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively. EGFRL858R|12 nM (IC50)|EGFRL858R/T790M|1 nM (IC50)
Osimertinib (AZD-9291) 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 (AZD-9291). 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[1].
The tumor-bearing mice are treated with Osimertinib (AZD-9291) (5 mg/kg/day) for one to two weeks. Within days of treatment, 5 of 5 C/L858R mice displays nearly 80% reduction in tumor volume by magnetic resonance imaging MRI after therapy with Osimertinib (AZD-9291), while 5 of 5 mice treated with vehicle shows tumor growth[1]. Osimertinib (AZD-9291) demonstrates improved rat PK, reduced hERG affinity, and improved IGF1R margins relative to the previously described compounds, and so this compound is selected for further investigation. Osimertinib (AZD-9291) also offers an additional degree of broader chemical and profile diversity when compared to the previously described lead compounds. Upon dosing Osimertinib (AZD-9291) in three efficacy models, The comparable efficacy is observed at relatively low doses (10 mg/kg per day). The excellent efficacy is also observed when Osimertinib (AZD-9291) is dosed at 5 mg/kg per day[2].
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. [2]. Finlay MR, et al. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistancemutations that spares the wild type form of the receptor. J Med Chem. 2014 Oct 23;57(20):8249-67.
Osimertinib dimesylate Preparation Products And Raw materials
Raw materials
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