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生物活性
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体外研究
与体外野生型相比，在突变EGFR 细胞系中AZD9291能更有效的抑制增殖
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体内研究
METTL7B is significantly increased in both mRNA and protein level in osimertinib -resistant xenografts as compared with those in osimertinib-sensitive xenografts. In LUAD CDX mouse model, combination treatment with GNC-siMETTL7B (6 mg siRNA per mouse equivalent) significantly suppresses tumor growth as compared with treatment of osimertinib (30 mg/kg) alone.
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激酶实验
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细胞实验
Cell lines: lung adenocarcinoma (LUAD) cell lines Concentrations: 0.001 -1 µM Incubation Time: 72 h Method: Cells are plated at a density of 3,000 cells/well in 96 well plates. Osimertinib is added to the medium and treated for 72 h. Cell viability assays are performed by Cell Counting Kit-8.
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动物实验
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不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
|  动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 |
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例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。
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参考文献
1. Song H, et al. Methyltransferase like 7B is a potential therapeutic target for reversing EGFR-TKIs resistance in lung adenocarcinoma. Mol Cancer. 2022 Feb 10;21(1):43.
2. Alessandro Leonetti, et al. Resistance mechanisms to osimertinib in EGFR-mutated non-small cell lung cancer. Br J Cancer . 2019 Oct;121(9):725-737.
分子式
C29H37N7O5S |
分子量
595.72 |
CAS号
1421373-66-1 |
储存方式
-20℃ |
溶剂（常温）
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DMSO
Soluble |
Water
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Ethanol
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体内溶解度
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Clinical Trial Information ( data from http://clinicaltrials.gov )
注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。
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