货号:A301515 同义名: VS-6062;PF-00562271
PF-562271(VS-6062)是一种高效、ATP竞争性和可逆的FAK和Pyk2激酶抑制剂,IC50值分别为1.5 nM和13 nM。
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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 non-receptor tyrosine kinase, can regulate the cytoskeleton and act as a scaffolding and signaling protein for other adhesion molecules. The expression of FAK and its phosphorylation status show a strong correlation with the invasive phenotype of aggressive human tumors. PF-562271 is a potent and selective inhibitor for FAK and Pyk2 with IC50 values of 1.5nM and 14nM (measured by recombinant kinase assay), respectively, displaying over 100-fold selectivity against the other kinases tested[1]. PF-562271 showed robust inhibition on p-FAK with IC50 of 5nM in an inducible cell-based assay. Oral administration of PF-562271 can inhibit p-FAK in a dose-dependent fashion with calculated EC50 of 93ng/ml in the tumor-bearing mice, which suggesting the pharmacodynamics of this compound. In vitro study showed that PF-562271 had antitumor efficacy or caused tumor regression in multiple human s.c. xenograft models, including BxPC3, LoVo, U87MG, H125, PC3M and BT474, with dose ranging in 25-100mg/kg according to different models[1]. |
作用机制 | PF-562271 can bind in the ATP-binding cleft of FAK and form two of the three H-bonds between PF-562271 and main-chain atoms in the kinase hinge region.[1] |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
KG-1 | Growth Inhibition Assay | IC50=5.74005 μM | SANGER | ||
KINGS-1 | Growth Inhibition Assay | IC50=12.3421 μM | SANGER | ||
KLE | Growth Inhibition Assay | IC50=28.9906 μM | SANGER | ||
KM12 | Growth Inhibition Assay | IC50=0.38557 μM | SANGER | ||
Dose | Mice: 12 mg/kg - 50 mg/kg[1] (p.o.) Monkey: 20 mg/kg - 80 mg/kg[2] (p.o.) |
Administration | p.o. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.97mL 0.39mL 0.20mL |
9.85mL 1.97mL 0.99mL |
19.70mL 3.94mL 1.97mL |
CAS号 | 717907-75-0 |
分子式 | C21H20F3N7O3S |
分子量 | 507.489 |
别名 | VS-6062;PF-00562271 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 65 mg/mL(128.08 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 |
IP 2% DMSO+2% Tween80+40% PEG300+water 10 mg/mL clear PO 0.5% CMC-Na 50 mg/mL suspension |