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{[ getRatePrice(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_am, item.pr_size) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} | 现货 | 咨询 | - + |
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产品名称 | FAK ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Defactinib | ✔ | 99%+ | |||||||||||||||||
NVP-TAE 226 |
++
FAK, IC50: 5.5 nM PYK2, IC50: 3.5 nM |
IGF-1R,Insulin Receptor | 98+% | ||||||||||||||||
PF-573228 |
+
FAK, IC50: 4 nM |
98% | |||||||||||||||||
Solanesol | ✔ | 90% +(HPLC) | |||||||||||||||||
PF-431396 |
++
FAK, IC50: 2 nM PYK2, IC50: 11 nM |
99%+ | |||||||||||||||||
PND-1186 |
++++
FAK, IC50: 1.5 nM |
99%+ | |||||||||||||||||
PF-562271 |
++++
FAK, IC50: 1.5 nM PYK2, IC50: 13 nM |
99%+ | |||||||||||||||||
GSK2256098 |
++++
FAK, Ki: 0.4 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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]. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 2341740-84-7 |
分子式 | C44H42F3N7O12 |
分子量 | 917.84 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
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 |