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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 |
Insulin Receptor,IGF-1R | 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。 |
靶点 |
|
描述 | FAK (focal adhesion kinase), a cytoplasmic non-receptor protein-tyrosine kinase, is associated with tumor progression through its modulation of various cellular processes including growth, survival, and migration. PND-1186 is reversible FAK inhibitor with IC50 value of 1.5 nM (measured by purified FAK kinase activity). It had IC50 value of about 100 nM for inhibition of p-FAK-Y397 in breast carcinoma cells. Exposure to 1 μM PND-1186 for 22 h restrains 4T1 breast carcinoma motility with only 40% closure, but no cell detachment or death observed, in wound healing assays. Low-concentration treatment with PND-1186 at 0.1-1 μM for 24-72 h caused dose- and time-dependent increased apoptosis of 4T1 cells cultured in suspension, but not under adherent condition. Consistent with this, PND-1186 could reduce the spheroid size of 3D-cultured 4T1 cells for 3 fold at concentration of 0.1 μM for 72 h with maximal effects achieved at 0.2 μM, which may due to the inhibition of tyrosine phosphorylation of both FAK and p130Cas under spheroid growth conditions but not 2D culture. Oral administration of PND-1186 at 100 mg/kg, BID, for 5 days inhibited 4T1 subcutaneous tumor growth in mice through induction of apoptosis[1]. |
Dose | Mice: 30 mg/kg, 100 mg/kg[2] (s.c.) |
Administration | s.c. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.99mL 0.40mL 0.20mL |
9.97mL 1.99mL 1.00mL |
19.94mL 3.99mL 1.99mL |
CAS号 | 1061353-68-1 |
分子式 | C25H26F3N5O3 |
分子量 | 501.501 |
别名 | VS-4718;SR-2516;SR-2156 |
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,2-8°C |
溶解度 |
DMSO: 35 mg/mL(69.79 mM),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 |
IP 2% DMSO+2% Tween80+30% PEG300+water 5 mg/mL clear PO 0.5% CMC-Na 30 mg/mL suspension |