Immunoway/AZD-9291 mesylate (Osimertinib，Mereletinib)/10mg 50mg 100mg/MC0941
市场价：
¥2800.00
美元价：
1400.00
联系Q Q：
3392242852
电话号码：
4000-520-616
电子邮箱：
info@ebiomall.com
商品介绍
AZD-9291 mesylate (Osimertinib，Mereletinib)
- Catalog No.：MC0941
- Data Sheet
- MSDS
- Support
- Description
- References ( 0 )
- Protocol
- CasNo：
- 1421373-66-1
- MolecularFormula：
- C29H37N7O5S
- Purity：
- >99%
- Target：
- EGFR
- IC50：
- IC50: 1 nM (EGFRL858R/T790M), 12 nM (EGFRL858R)[1]
- In Vitro：
- AZD-9291 (AZD9291) 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 AZD-9291. 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].
- In Vivo：
- The tumor-bearing mice are treated with 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 AZD-9291, while 5 of 5 mice treated with vehicle shows tumor growth[1]. 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. AZD-9291 also offers an additional degree of broader chemical and profile diversity when compared to the previously described lead compounds. Upon dosing 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 AZD-9291 is dosed at 5 mg/kg per day[2].
- Fields：
- AZD-9291 is a potent and selective mutated forms EGFR inhibitor(Exon 19 deletion EGFR IC50=12.92 nM, L858R/T790M EGFR IC50= 11.44 nM, wild type EGFR IC50= 493.8 nM).
- Specificity：
- Target: EGFR . Fields: AZD-9291 is a potent and selective mutated forms EGFR inhibitor(Exon 19 deletion EGFR IC50=12.92 nM, L858R/T790M EGFR IC50= 11.44 nM, wild type EGFR IC50= 493.8 nM).
- Source：
- Rabbit
- Dilution：
- IC50: 1 nM (EGFRL858R/T790M), 12 nM (EGFRL858R)[1]
- Concentration：
- >99%
- Storage Stability：
- 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
- Other Name：
- Mereletinib mesylate; EGFR inhibitor; AZD9291 mesylate; AZD 9291 mesylate，Tagrisso
- MolecularWeight(Da)：
- 595.71
- 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
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