生物活性

ASP8273 is a small molecule, irreversible TKI inhibitor that inhibits the kinase activity of EGFR mutations including T790M, with limited activity against EGFR wild-type NSCLC. In the in vitro enzymatic and cell-based assays, ASP8273 were evaluated against EGFR mutantsand WT EGFR. ASP8273, a mutant-selective irreversibleTKI inhibitor currently in clinical trials, inhibits the kinase activity ofEGFR mutations including T790M, with limited activity against EGFR wild-type(WT) NSCLC.

Growthinhibition of ASP8273[1][2][3]

体外研究

体内研究

激酶实验

细胞实验

动物实验

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）

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。

参考文献

[1] Hidski Sakagami SK, Hiroko Yamamoto, Hiroaki Tanaka, Takahiro Matsuya,, Masamichi Mori HK, Masatoshi Yuri, Masaaki Hrano, and Sadao Kuromitsu. Abstract 1728: ASP8273, a novel mutant-selective irreversible EGFR inhibitor, inhibits growth of nonsmall cell lung cancer (NSCLC) cells with EGFR activating and T790M resistance mutations. Cancer Res. 2014;74(19 Supplement):1728.
[2] Satoshi Konagai HS, Hiroko Yamamoto, Hiroaki Tanaka, Takahiro Matsuya, Shinya Mimasu, YT, Masamichi Mori, Hiroyuki Koshio, Masaaki Hirano, Sadao Kuromitsu, and, Takeuchi M. Abstract 2586: ASP8273 selectively inhibits mutant EGFR signal pathway and induces tumor shrinkage in EGFR mutated tumor models. Cancer Res. 2015; 75(15 Supplement):25.
[3] Ou SH, Soo RA. Dacomitinib in lung cancer: a "lost generation" EGFR tyrosine-kinase inhibitor from a bygone era? Drug design, development and therapy. 2015;9:5641-5653.

体内溶解度

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。

相关化合物库

使用AMQUAR产品发表文献后请联系我们