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PF-562271 Besylate
别名: PF-00562271 Besylate
PF-562271 Besylate是PF-562271的苯磺酸盐，是一种有效的，ATP竞争性，可逆的FAK抑制剂，IC50为1.5 nM，作用于Pyk2比作用于FAK效果低10倍左右，比作用于其他蛋白激酶（除了一些CDKs）选择性高100倍以上。Phase 1。
PF-562271 Besylate Chemical Structure
CAS: 939791-38-5
产品质控
批次：
纯度：
99.32%
99.32
PF-562271 Besylate相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息(PMID) |
|---|---|---|---|---|---|
| human SNU-387 cell | Growth inhibition assay | Inhibition of human SNU-387 cell growth in a cell viability assay, IC50=2.5282 μM | |||
| human MDA-MB-231 cell | Growth inhibition assay | Inhibition of human MDA-MB-231 cell growth in a cell viability assay, IC50=2.49572 μM | |||
| human DU-145 cell | Growth inhibition assay | Inhibition of human DU-145 cell growth in a cell viability assay, IC50=2.49118 μM | |||
| human MFE-296 cell | Growth inhibition assay | Inhibition of human MFE-296 cell growth in a cell viability assay, IC50=2.47792 μM | |||
| human DU-4475 cell | Growth inhibition assay | Inhibition of human DU-4475 cell growth in a cell viability assay, IC50=2.14759 μM | |||
| human NCI-H460 cell | Growth inhibition assay | Inhibition of human NCI-H460 cell growth in a cell viability assay, IC50=2.04839 μM | |||
| human U251 cell | Growth inhibition assay | Inhibition of human U251 cell growth in a cell viability assay, IC50=1.74031 μM | |||
| human EW-13 cell | Growth inhibition assay | Inhibition of human EW-13 cell growth in a cell viability assay, IC50=1.63466 μM | |||
| human SW1710 cell | Growth inhibition assay | Inhibition of human SW1710 cell growth in a cell viability assay, IC50=1.62628 μM | |||
| human MZ1-PC cell | Growth inhibition assay | Inhibition of human MZ1-PC cell growth in a cell viability assay, IC50=1.62312 μM | |||
| human CGTH-W-1 cell | Growth inhibition assay | Inhibition of human CGTH-W-1 cell growth in a cell viability assay, IC50=1.61679 μM | |||
| human BC-1 cell | Growth inhibition assay | Inhibition of human BC-1 cell growth in a cell viability assay, IC50=1.61664 μM | |||
| human HSC-2 cell | Growth inhibition assay | Inhibition of human HSC-2 cell growth in a cell viability assay, IC50=1.5395 μM | |||
| human ST486 cell | Growth inhibition assay | Inhibition of human ST486 cell growth in a cell viability assay, IC50=1.53278 μM | |||
| human AGS cell | Growth inhibition assay | Inhibition of human AGS cell growth in a cell viability assay, IC50=1.52124 μM | |||
| human SIG-M5 cell | Growth inhibition assay | Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=1.48487 μM | |||
| human HUTU-80 cell | Growth inhibition assay | Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=1.44886 μM | |||
| human SK-UT-1 cell | Growth inhibition assay | Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50=1.44647 μM | |||
| human KYSE-150 cell | Growth inhibition assay | Inhibition of human KYSE-150 cell growth in a cell viability assay, IC50=1.35236 μM | |||
| human CAL-62 cell | Growth inhibition assay | Inhibition of human CAL-62 cell growth in a cell viability assay, IC50=1.31909 μM | |||
| human MES-SA cell | Growth inhibition assay | Inhibition of human MES-SA cell growth in a cell viability assay, IC50=1.30682 μM | |||
| human BPH-1 cell | Growth inhibition assay | Inhibition of human BPH-1 cell growth in a cell viability assay, IC50=1.28766 μM | |||
| human NKM-1 cell | Growth inhibition assay | Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=1.27506 μM | |||
| human AN3-CA cell | Growth inhibition assay | Inhibition of human AN3-CA cell growth in a cell viability assay, IC50=1.21867 μM | |||
| human CAL-33 cell | Growth inhibition assay | Inhibition of human CAL-33 cell growth in a cell viability assay, IC50=1.12938 μM | |||
| NCI-H810 cell | Growth inhibition assay | Inhibition of human NCI-H810 cell growth in a cell viability assay, IC50=1.10776 μM | |||
| human 8305C cell | Growth inhibition assay | Inhibition of human 8305C cell growth in a cell viability assay, IC50=1.09904 μM | |||
| human KYSE-270 cell | Growth inhibition assay | Inhibition of human KYSE-270 cell growth in a cell viability assay, IC50=1.04714 μM | |||
| ALL-PO cell | Growth inhibition assay | Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=1.01584 μM | |||
| human BCPAP cell | Growth inhibition assay | Inhibition of human BCPAP cell growth in a cell viability assay, IC50=1.01288 μM | |||
| human RT-112 cell | Growth inhibition assay | Inhibition of human RT-112 cell growth in a cell viability assay, IC50=0.9846 μM | |||
| human NCI-H650 cell | Growth inhibition assay | Inhibition of human NCI-H650 cell growth in a cell viability assay, IC50=0.83154 μM | |||
| human IGROV-1 cell | Growth inhibition assay | Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=0.81038 μM | |||
| human MG-63 cell | Growth inhibition assay | Inhibition of human MG-63 cell growth in a cell viability assay, IC50=0.80637 μM | |||
| human COLO-829 cell | Growth inhibition assay | Inhibition of human COLO-829 cell growth in a cell viability assay, IC50=0.76176 μM | |||
| human COLO-205 cell | Growth inhibition assay | Inhibition of human COLO-205 cell growth in a cell viability assay, IC50=0.48658 μM | |||
| human KM12 cell | Growth inhibition assay | Inhibition of human KM12 cell growth in a cell viability assay, IC50=0.38557 μM | |||
| human SW982 cell | Growth inhibition assay | Inhibition of human SW982 cell growth in a cell viability assay, IC50=0.3282 μM | |||
| MV-4-11 cell | Growth inhibition assay | Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=0.2766 μM | |||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | PF-562271 Besylate是PF-562271的苯磺酸盐，是一种有效的，ATP竞争性，可逆的FAK抑制剂，IC50为1.5 nM，作用于Pyk2比作用于FAK效果低10倍左右，比作用于其他蛋白激酶（除了一些CDKs）选择性高100倍以上。Phase 1。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | 在重组酶实验中, PF-562271 Besylate选择性抑制FAK 和 Pyk2 酪氨酸激酶活性，IC50分别为1.5 nM 和14 nM。在细胞实验中，PF-562271 作用于FAK的IC50值为5 nM，比作用于其他激酶靶点选择性更高。[1] 在二维培养中，PF-562271 抑制FAK WT,FAK−/− 和FAK 激酶缺乏(KD)的细胞增殖，IC50分别为3.3 μM, 2.08 μM 和 2.01 μM。[2] | |||
|---|---|---|---|---|
| 激酶实验 | 重组激酶实验和酶动力学 | |||
| 纯化激活的FAK激酶域 (第 410–689位氨基酸)与 50 μM ATP ，和每孔 10 μg Glu 和 Tyr, p(Glu/Tyr)随机肽聚合物,在激酶buffer [50 mM HEPES (pH 7.5), 125 mM NaCl, 和 48 mM MgCl2] 中反应15分钟。使用从1 μM连续稀释的PF-562271 进行p(Glu/Tyr)磷酸化。实验中每种实验浓度重复三次。使用通用 抗磷酸酪氨酸 (PY20) 抗体和随后的辣根过氧化物酶（HRP）标记的羊抗鼠IgG抗体检测p(Glu/Tyr) 的磷酸化。加入HRP 底物，加入终止液(2 M H2SO4)，在450 nm处测定吸光值。使用Hill-Slope 模型测定IC50值。使用KinaseProfiler 选择性筛选服务系统通过UpState生物技术进行广谱激酶选择谱研究。 | ||||
| 细胞实验 | 细胞系 | 鳞状细胞癌(SCC) | ||
| 浓度 | 0 到1 μM | |||
| 孵育时间 | 72小时 | |||
| 方法 | 细胞接种48小时后，加入PF-562271。加入冰冻25% 三氯乙酸 (TCA) 溶液，混合细胞，3天后，使用 Sulforhodamine B(SRB) 染料染色。使用1% 冰醋酸冲洗实验板，烘干，然后再悬浮在10 mM Tris buffer, pH 10.5中，然后在 540 nm处测定吸光值。拟合曲线，使用GraphPad Prism 4 软件从6次重复测定中获得IC50值。 |
|||
| 体内研究(In Vivo) | ||
| 体内研究活性 | PF-562271 Besylate作用于一些人类皮下移植瘤模型，抑制肿瘤生长，这种作用存在剂量依赖性，且产生最大肿瘤抑制效果，按25 到 50 mg/kg剂量作用于PC-3M, BT474, BxPc3, 和LoVo细胞，每天两次，抑制达78%到94%，没有发生体重降低，生病或死亡。[1]PF-562271 按25 mg/kg剂量口服处理皮下和骨转移PC3M-LUC-5233移植瘤模型，显著降低肿瘤进展。[3] | |
|---|---|---|
| 动物实验 | Animal Models | PC-3M, BT474, BxPc3, LoVo, U87MG, H125 和H460细胞皮下注射到无胸腺雌性小鼠右侧 |
| Dosages | ≤100 mg/kg | |
| Administration | 口服处理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00666926 | Completed | Head and Neck Neoplasm|Prostatic Neoplasm|Pancreatic Neoplasm |
Verastem Inc. |
December 2005 | Phase 1 |
|
化学信息&溶解度
| 分子量 | 665.66 | 分子式 | C21H20F3N7O3S.C6H6O3S |
| CAS号 | 939791-38-5 | SDF | Download PF-562271 Besylate SDF |
| Smiles | CN(C1=C(C=CC=N1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC4=C(C=C3)NC(=O)C4)S(=O)(=O)C.C1=CC=C(C=C1)S(=O)(=O)O | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
4-Methylpyridine : 25 mg/mL (37.55 mM) DMSO : 0.4 mg/mL ( (0.6 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解配方 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | |||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 1:
We are planning both in vitro and in vivo experiments and want to know how to reconstitute the drug for these purposes?
回答：
PF-00562271 has poor solubility in DMSO and water. Its solubility in DMSO is only 0.4mg/ml. In a previous literature report (http://www.ncbi.nlm.nih.gov/pubmed/18339875), the author used 5% Gelucire to formulate the compound. You can also consider other co-solvents such as PEG400, CMC, Tween80, and Captisol.
问题 2:
Can you provide with a few common vehicles for PF-00562271, S2672 for use as oral gavage?
回答：
S2672 PF-00562271 can be dissolved in 0.5% CMC Na at 30 mg/ml as a suspension. If 4% DMSO can be used in your experiment, it will help dissolving the suspension more homogeneously.
