store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 432 | 现货 | ||
5 mg | ¥ 977 | 现货 | ||
10 mg | ¥ 1,530 | 现货 | ||
25 mg | ¥ 2,450 | 现货 | ||
50 mg | ¥ 3,480 | 现货 | ||
100 mg | ¥ 4,960 | 现货 | ||
500 mg | ¥ 6,913 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,070 | 现货 |
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 |
分子量 | 507.49 |
分子式 | C21H20F3N7O3S |
CAS No. | 717907-75-0 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (183.3 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9705 mL | 9.8524 mL | 19.7048 mL | 49.2621 mL |
5 mM | 0.3941 mL | 1.9705 mL | 3.941 mL | 9.8524 mL | |
10 mM | 0.197 mL | 0.9852 mL | 1.9705 mL | 4.9262 mL | |
20 mM | 0.0985 mL | 0.4926 mL | 0.9852 mL | 2.4631 mL | |
50 mM | 0.0394 mL | 0.197 mL | 0.3941 mL | 0.9852 mL | |
100 mM | 0.0197 mL | 0.0985 mL | 0.197 mL | 0.4926 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 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 μL,一共给药动物10 只,您使用的配方为5% 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 μL DMSO (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:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
PF-562271 717907-75-0 Angiogenesis Cell Cycle/Checkpoint Cytoskeletal Signaling Tyrosine Kinase/Adaptors FAK PYK2 CDK PF562271 Cancer PTK2 Ewing Antitumor Pyk2 PTK2 protein tyrosine kinase 2 Sarcoma PF 562271 inhibit Breast Focal adhesion kinase VS 6062 VS6062 Inhibitor Proline-rich tyrosine kinase 2 VS-6062 inhibitor