BI-3663 is a highly selective PTK2/FAK PROTAC (DC 50 =30 nM), with Cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC 50 of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 (HY-124625) linked to Pomalidomide (HY-10984) with a linker. Anti-cancer activity.
性状
Solid
IC50 & Target[1][2]
PTK2/FAK 18 nM (IC50) Cereblon
体外研究(In Vitro)
BI-3663 potently degrades PTK2 in Hep3B2.1-7 cells, and A549 cells, with pDC50s of 7.6 and 7.9, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
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
参考文献
[1]. Popow J, et al. Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions. J Med Chem. 2019 Mar 14;62(5):2508-2520.
溶解度数据
In Vitro: DMSO : 300 mg/mL (326.85 mM; Need ultrasonic)配制储备液