产品描述

Osimertinib is a small molecule tyrosine kinase receptor inhibitor and antineoplastic agent that is used in the therapy of selected forms of advanced non-small cell lung cancer (NSCLC).

靶点活性

EGFR (Exon 19 deletion),12.92nM

EGFR (L858R/T790M ),1nM

应用领域

Cancer

实验溶液

1% DMSO+30% PEG 300+dd Water: 30

体外活性

在突变EGFR细胞系中，AZD9291能够有效得抑制细胞增殖。

体内活性

EGFRm+（PC9）和EGFRm+/ T790M（H1975）肿瘤模型肿瘤中，口服 AZD9291（5mg/kg）能够抑制AKT和ERK信号通路及体内的EGFR磷酸化，引起肿瘤的消退

细胞实验

AZD9291 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. PC-9 cells are seeded into T75 flasks (5×105 cells/flask) in RPMI growth media and incubated at 37°C, 5% CO2. The following day the media is replaced with media supplemented with a concentration of EGFR inhibitor equal to the EC50 concentration predetermined in PC-9 cells. Media changes are carried out every 2-3 days and resistant clones allowed to grow to 80% confluency prior to the cells being trypsinised and reseeded at the original seeding density in media containing twice the concentration of EGFR inhibitor. Dose escalations are continued until a final concentration of 1.5 μM Gefitinib, 1.5 μM Afatinib, 1.5 μM WZ4002 or 160 nM AZD-9291 are achieved[1].

动物实验

动物模型：Mice

分子量

499.61

分子式

C28H33N7O2

CAS

1421373-65-0

溶解度

DMSO: 92 mg/mL (184.1 mM)

Ethanol: 40 mg/mL (80.1 mM)

Water: <1 mg/mL

（ < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

3 years  -20℃  powder

2 years  -80℃  In solvent

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.