Apratastat (TMI-005) is an orally active, non-selective and reversible TACE/MMPs inhibitor, can inhibit inhibit the release of TNF-α. Apratastat has the potential to overcome radiotherapy-resistance in non-small cell lung cancer (NSCLC).
性状
Solid
IC50 & Target[1][2]
MMP
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Shu C, et al. Pharmacokinetic-pharmacodynamic modeling of apratastat: a population-based approach. J Clin Pharmacol. 2011 Apr;51(4):472-81.[2]. Ieguchi K, et al. Savior or not: ADAM17 inhibitors overcome radiotherapy-resistance in non-small cell lung cancer. J Thorac Dis. 2016 Aug;8(8):E813-5.
溶解度数据
In Vitro: DMSO : 41.4 mg/mL (99.88 mM; Need ultrasonic and warming)配制储备液