Osimertinib dimesylate
- CAS No.
- 2070014-82-1
- Chemical Name:
- Osimertinib dimesylate
- Synonyms
- Osimertinib dimesylate
- CBNumber:
- CB05419799
- Molecular Formula:
- C29H37N7O5S
- Molecular Weight:
- 595.72
- MDL Number:
- MOL File:
- 2070014-82-1.mol
Osimertinib dimesylate price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
ChemScene | CS-3405 | Osimertinibdimesylate 99.96% | 2070014-82-1 | 5mg | $60 | 2021-12-16 | Buy |
ChemScene | CS-3405 | Osimertinibdimesylate 99.96% | 2070014-82-1 | 10mg | $70 | 2021-12-16 | Buy |
ChemScene | CS-3405 | Osimertinibdimesylate 99.96% | 2070014-82-1 | 50mg | $100 | 2021-12-16 | Buy |
ChemScene | CS-3405 | Osimertinibdimesylate 99.96% | 2070014-82-1 | 100mg | $120 | 2021-12-16 | Buy |
ChemScene | CS-3405 | Osimertinibdimesylate 99.96% | 2070014-82-1 | 200mg | $140 | 2021-12-16 | Buy |
Osimertinib dimesylate Chemical Properties,Uses,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
Osimertinib dimesylate Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
Henan Fengda Chemical Co., Ltd | +86-371-86557731 +86-13613820652 | info@fdachem.com | China | 16805 | 58 |
Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
Tianjin Branch Chong pharmaceutical intermediates Co., Ltd. | 022-60116533 13207668525 | saleskc@scipharmacn.com | China | 886 | 58 |
ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 | sales-cpd@caerulumpharma.com | China | 3421 | 58 |
Cangzhou Enke Pharma-tech Co., Ltd. | 0317-5296180 15533709196 | sale@enkepharma.com | China | 1649 | 55 |
Beijing Solarbio Science & Tecnology Co., Ltd. | 010-50973130 4009686088 | 3193328036@qq.com | China | 29797 | 68 |
Fan De(Beijing) Biotechnology Co., Ltd. | 15911056312 | liming@bio-fount.com | China | 9730 | 58 |
ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11289 | 58 |