Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PF-562271 besylate (PF-00562271 Besylate) 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 | ¥ 428 | 现货 | ||
2 mg | ¥ 632 | 现货 | ||
5 mg | ¥ 995 | 现货 | ||
10 mg | ¥ 1,730 | 现货 | ||
25 mg | ¥ 2,960 | 现货 | ||
50 mg | ¥ 4,330 | 现货 | ||
100 mg | ¥ 6,180 | 现货 | ||
500 mg | ¥ 12,600 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,380 | 现货 |
产品描述 | PF-562271 besylate (PF-00562271 Besylate) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. |
靶点活性 | FAK:1.5 nM |
体外活性 | PF-562271 shows the selective inhibitory effects on FAK and Pyk2 tyrosine kinase activity with IC50 of 1.5 nM and 14 nM, respectively. And in cell-based assays, the IC50 of PF-562271 is shown to be 5 nM for FAK, which is more selective compared to other kinase targets. [1] In 2 dimensional (2D) cultures, PF-562271 results in a dose-dependent cell proliferation inhibition in FAK WT, FAK?/? and FAK kinase-deficient (KD) cells with IC50 of 3.3 μM, 2.08 μM and 2.01 μM, respectively. [2] |
体内活性 | In several human s.c. xenograft models, PF-562271 exhibits dose-dependent tumor growth inhibition, and produces maximum tumor inhibition for PC-3M, BT474, BxPc3, and LoVo ranging from 78% to 94% inhibition at doses of 25 to 50 mg/kg twice daily, without weight loss, morbidity, or death. [1] PF-562271 (25 mg/kg by p.o.) leads to a significant decrease in tumor progression in both subcutaneous and bone metastasis PC3M-luc-C6 xenograft models. [3] In a Huh7.5 hepatocellular carcinoma xenograft model, combination therapy of sunitinib and PF-562271 targets angiogenesis and tumor aggressiveness, and produces more significant anti-tumor effect than single agent by blocking tumor growth and impacting the ability of the tumor to recover upon withdrawal of the therapy. [4] |
激酶实验 | Recombinant kinase assay and enzyme kinetics : Briefly, 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 minutes. Phosphorylation of p(Glu/Tyr) is challenged with serially diluted PF-562271 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. Broad kinase selectivity profiling is performed in house and by using the KinaseProfiler Selectivity Screening Service available through UpState Biotechnology. |
细胞实验 | Cells are plated for 48 hours before addition of PF-562271. After 3 days cells are fixed by addition of ice cold 25% trichloroacetic acid (TCA) solution prior to staining with Sulforhodamine B (SRB) dye solution. Plates are washed with 1% glacial acetic acid, air-dried and resuspended in 10 mM Tris buffer, pH 10.5 before reading absorbance at 540 nm. Curve fitting and generation of IC50 values is carried out using GraphPad Prism 4 software from six replicates.(Only for Reference) |
别名 | PF-00562271 Besylate |
分子量 | 665.66 |
分子式 | C21H20F3N7O3S·C6H6O3S |
CAS No. | 939791-38-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 12 mg/mL (18 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.5023 mL | 7.5113 mL | 15.0227 mL | 37.5567 mL |
5 mM | 0.3005 mL | 1.5023 mL | 3.0045 mL | 7.5113 mL | |
10 mM | 0.1502 mL | 0.7511 mL | 1.5023 mL | 3.7557 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 besylate 939791-38-5 Angiogenesis Cell Cycle/Checkpoint Cytoskeletal Signaling Tyrosine Kinase/Adaptors FAK PYK2 CDK Pyk2 Inhibitor Focal adhesion kinase inhibit PF562271 besylate PF 562271 besylate VS-6062 besylate PTK2 PF-00562271 Besylate Proline-rich tyrosine kinase 2 PTK2 protein tyrosine kinase 2 inhibitor