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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
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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
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-3405
Product name
Osimertinibdimesylate
Purity
99.96%
Packaging
5mg
Price
$60
Updated
2021/12/16
ChemScene
Product number
CS-3405
Product name
Osimertinibdimesylate
Purity
99.96%
Packaging
10mg
Price
$70
Updated
2021/12/16
ChemScene
Product number
CS-3405
Product name
Osimertinibdimesylate
Purity
99.96%
Packaging
50mg
Price
$100
Updated
2021/12/16
ChemScene
Product number
CS-3405
Product name
Osimertinibdimesylate
Purity
99.96%
Packaging
100mg
Price
$120
Updated
2021/12/16
ChemScene
Product number
CS-3405
Product name
Osimertinibdimesylate
Purity
99.96%
Packaging
200mg
Price
$140
Updated
2021/12/16
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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

Preparation Products

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Osimertinib dimesylate Suppliers

Tianjin Branch Chong pharmaceutical intermediates Co., Ltd.
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022-60116533 13207668525
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China
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683
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Shanghai EFE Biological Technology Co., Ltd.
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Cangzhou Enke Pharma-tech Co., Ltd.
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Beijing Solarbio Science & Tecnology Co., Ltd.
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Heze Development Zone chuangli Chemical Co., Ltd.
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Fan De(Beijing) Biotechnology Co., Ltd.
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TargetMol Chemicals Inc.
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marketing@targetmol.com
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United States
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InvivoChem
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ChemeGen(Shanghai) Biotechnology Co.,Ltd.
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18818260767
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QQ 3610331285
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