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PF-562271

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产品编号 T2465Cas号 717907-75-0
别名 PF562271, PF 562271

PF-562271 是一种可逆的,有效的,ATP 竞争性的 FAK (IC50:1.5 nM)和 Pyk2 (IC50:13 nM)激酶抑制剂。

PF-562271

PF-562271

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纯度: 100%
产品编号 T2465 别名 PF562271, PF 562271Cas号 717907-75-0

PF-562271 是一种可逆的,有效的,ATP 竞争性的 FAK (IC50:1.5 nM)和 Pyk2 (IC50:13 nM)激酶抑制剂。

规格价格库存数量
1 mg
¥ 432
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5 mg
¥ 977
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10 mg
¥ 1,530
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25 mg
¥ 2,450
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50 mg
¥ 3,480
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100 mg
¥ 4,960
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500 mg
¥ 6,913
现货
1 mL x 10 mM (in DMSO)
¥ 1,070
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产品介绍

生物活性
产品描述
PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM).
靶点活性
FAK:1.5 nM, PYK2:13 nM
体外活性
在胫骨植入MDA-MB-231细胞的大鼠中,口服 PF-562271(5 mg/kg),引起骨钙素和松质骨增加,从而使肿瘤细胞生长减缓.在携带H125肺部异种移植肿瘤、异种移植PC3M-luc-C6的小鼠模型中,口服 PF-562271 (25 mg/kg)抑制肿瘤细胞生长,引起细胞凋亡.在U87 mg的小鼠中,PF-562271(口服< 33 mg/kg)能够以时间和剂量依赖的方式抑制肿瘤中FAK磷酸化.在BxPc3异种移植小鼠、PC3-M异种移植小鼠中口服 PF-562271(50 mg/kg),能够抑制肿瘤生长.
体内活性
PF-562271能够结合在ATP与FAK结合的部位,并在激酶铰链区形成抑制剂与主链原子之间的氢键。在鸡胚绒毛尿囊膜中,PF-562271(1 nM )阻断bFGF刺激的血管生成。在PC3-M细胞中,PF-562271(3.3 μM)能够使细胞停止在G1期。对于A431 细胞,PF-562271(250 nM )能够抑制细胞侵入胶原蛋白。
激酶实验
The purified-activated FAK kinase domain (amino acid 410-689) is reacted with 50 μM ATP and 10 μg per well of a random peptide polymer of Glu and Tyr, p(Glu/Tyr), in kinase buffer (50 mM HEPES pH 7.5, 125 mM NaCl, and 48 mM MgCl2) for 15 min. Phosphorylation of p(Glu/Tyr) is challenged with serially diluted compound at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is tested in triplicate. Phosphorylation of p(Glu/Tyr) is detected with a general antiphospho-tyrosine (PY20) antibody followed by horseradish peroxidase (HRP)-conjugated goat anti-mouse IgG antibody. HRP substrate is added, and absorbance readings at 450 nm are obtained after addition of stop solution (2 M H2SO4). IC50 values are determined using the Hill-Slope Model[1].
细胞实验
PF-562271 (Haoyuan Chemexpress Co., Ltd.) is dissolved in DMSO and stored, and then diluted with appropriate media before use[2]. Ewing sarcoma cells are plated in 10-cm dishes, allowed to adhere for 24 hours, and then treated with PF-562271, PD0325901, or Dasatinib. ATP content is measured as a surrogate for cell number using the CellTiter-Glo Luminescent Cell Viability Assay. Luminescence readings are obtained using the FLUOstar Omega microplate reader. For experiments with small-molecule treatment, 1.25×103 Ewing sarcoma cells are seeded in each well and treated with a range of concentrations. IC50 values are calculated from ATP measurements obtained after 3 days of treatment using log-transformed, normalized data in GraphPad Prism 5.0. Cell lines are also treated with compound in 6-cm dishes, trypsinized, and counted by light microscopy using trypan blue exclusion. For experiments using shRNA-transduced cells, 1.25×103 cells are seeded per well into 384-well plates on day 3 posttransduction. ATP content is measured on days 3, 6, and 8 posttransduction[2].
别名PF562271, PF 562271
化学信息
分子量507.49
分子式C21H20F3N7O3S
CAS No.717907-75-0
SmilesCN(c1ncccc1CNc1nc(Nc2ccc3NC(=O)Cc3c2)ncc1C(F)(F)F)S(C)(=O)=O
密度1.54
储存&溶解度
存储store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 93 mg/mL (183.25 mM), Sonication is recommended.
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM1.9705 mL9.8524 mL19.7048 mL98.5241 mL
5 mM0.3941 mL1.9705 mL3.9410 mL19.7048 mL
10 mM0.1970 mL0.9852 mL1.9705 mL9.8524 mL
20 mM0.0985 mL0.4926 mL0.9852 mL4.9262 mL
50 mM0.0394 mL0.1970 mL0.3941 mL1.9705 mL
100 mM0.0197 mL0.0985 mL0.1970 mL0.9852 mL

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TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

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