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BI-3663

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Chemical Structure| 2341740-84-7 同义名 : -
CAS号 : 2341740-84-7
货号 : A1148283
分子式 : C44H42F3N7O12
纯度 : 99%
分子量 : 917.84
MDL号 : MFCD31813809
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 300 mg/mL(326.85 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 BI-3663 is a CRBN-recruiting PROTAC targeting on PTK2. BI-3663 could degrade PTK2 with pDC50 values/Dmax[%] values of 7.6/90, 6.6/50, 7.9/96, 7.5/89, 7.5/89, 6.4/30, 8.5/95, 7.9/90, 6.8/79, 7.3/93 and 7.9/93 for degradation of PTK2 in SNU-387, HUH-1, Hep3B2.1-7, HepG2, SK-Hep-1, HLF, SNU-398, HUCCT1, HLE, HuH-7 and SNU-423 cell lines. Also, it exhibited potency against proliferation of SNU-387, HUH-1, Hep3B2.1-7, HepG2, SK-Hep-1, HLF, SNU-398, HUCCT1, HLE, HuH-7 and SNU-423 cells with pIC50 values of <4.6, 4.6, 4.6, <4.6, 5.8, <4.6, <4.6, <4.6, <4.6, <4.6 and 4.7, respectively. The combined treatment of Cyclosporine A with BI-3663 could potentiate PTK2 degradation due to Cyclosporine A (10μM) working as a substrate of several drug transporters to saturate these transporters at high concentrations[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.09mL

0.22mL

0.11mL

5.45mL

1.09mL

0.54mL

10.90mL

2.18mL

1.09mL
参考文献

[1]Popow J, Arnhof H, 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.