Osimertinib mesylate

产品说明书

Print
Chemical Structure| 1421373-66-1 同义名 : AZD-9291 甲磺酸盐 ;AZD-9291 mesylate; Mereletinib mesylate
CAS号 : 1421373-66-1
货号 : A188322
分子式 : C29H37N7O5S
纯度 : 98% (Content MsOH 15.2-18.2%)
分子量 : 595.71
MDL号 : MFCD28137994
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 12 mg/mL(20.14 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • EGFR/ErbB1
描述 Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible EGFR inhibitor selective for mutant forms, with an IC50 of 12 nM against the L858R mutation and 1 nM against the L858R/T790M mutation. Otherwise, Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
作用机制 Osimertinib may bind to T790M EGFR kinase in the ATP-binding domain (such as T790M and C797S).[3]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.68mL

0.34mL

0.17mL

8.39mL

1.68mL

0.84mL

16.79mL

3.36mL

1.68mL
参考文献

[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]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.