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- 生物試劑
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實驗
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 細胞核與細胞漿蛋白抽提試劑盒
- 免疫磁珠
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲液)
- 磷酸酶抑制劑Cocktail
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PF-562271 Besylate
別名: PF-00562271 Besylate
PF-562271 Besylate是PF-562271的苯磺酸鹽，是一種有效的，ATP競爭性，可逆的FAK抑制劑，IC50為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）選擇性高100倍以上。Phase 1。
PF-562271 Besylate Chemical Structure
CAS: 939791-38-5
產(chǎn)品質控
批次：
純度：
99.32%
99.32
PF-562271 Besylate相關產(chǎn)品
相關信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息(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 | |||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | PF-562271 Besylate是PF-562271的苯磺酸鹽，是一種有效的，ATP競爭性，可逆的FAK抑制劑，IC50為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）選擇性高100倍以上。Phase 1。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | 在重組酶實驗中, PF-562271 Besylate選擇性抑制FAK 和 Pyk2 酪氨酸激酶活性，IC50分別為1.5 nM 和14 nM。在細胞實驗中，PF-562271 作用于FAK的IC50值為5 nM，比作用于其他激酶靶點選擇性更高。[1] 在二維培養(yǎng)中，PF-562271 抑制FAK WT,FAK?/? 和FAK 激酶缺乏(KD)的細胞增殖，IC50分別為3.3 μM, 2.08 μM 和 2.01 μM。[2] | |||
|---|---|---|---|---|
| 激酶實驗 | 重組激酶實驗和酶動力學 | |||
| 純化激活的FAK激酶域 (第 410–689位氨基酸)與 50 μM ATP ，和每孔 10 μg Glu 和 Tyr, p(Glu/Tyr)隨機肽聚合物,在激酶buffer [50 mM HEPES (pH 7.5), 125 mM NaCl, 和 48 mM MgCl2] 中反應15分鐘。使用從1 μM連續(xù)稀釋的PF-562271 進行p(Glu/Tyr)磷酸化。實驗中每種實驗濃度重復三次。使用通用 抗磷酸酪氨酸 (PY20) 抗體和隨后的辣根過氧化物酶（HRP）標記的羊抗鼠IgG抗體檢測p(Glu/Tyr) 的磷酸化。加入HRP 底物，加入終止液(2 M H2SO4)，在450 nm處測定吸光值。使用Hill-Slope 模型測定IC50值。使用KinaseProfiler 選擇性篩選服務系統(tǒng)通過UpState生物技術進行廣譜激酶選擇譜研究。 | ||||
| 細胞實驗 | 細胞系 | 鱗狀細胞癌(SCC) | ||
| 濃度 | 0 到1 μM | |||
| 孵育時間 | 72小時 | |||
| 方法 | 細胞接種48小時后，加入PF-562271。加入冰凍25% 三氯乙酸 (TCA) 溶液，混合細胞，3天后，使用 Sulforhodamine B(SRB) 染料染色。使用1% 冰醋酸沖洗實驗板，烘干，然后再懸浮在10 mM Tris buffer, pH 10.5中，然后在 540 nm處測定吸光值。擬合曲線，使用GraphPad Prism 4 軟件從6次重復測定中獲得IC50值。 |
|||
| 體內研究(In Vivo) | ||
| 體內研究活性 | PF-562271 Besylate作用于一些人類皮下移植瘤模型，抑制腫瘤生長，這種作用存在劑量依賴性，且產(chǎn)生最大腫瘤抑制效果，按25 到 50 mg/kg劑量作用于PC-3M, BT474, BxPc3, 和LoVo細胞，每天兩次，抑制達78%到94%，沒有發(fā)生體重降低，生病或死亡。[1]PF-562271 按25 mg/kg劑量口服處理皮下和骨轉移PC3M-LUC-5233移植瘤模型，顯著降低腫瘤進展。[3] | |
|---|---|---|
| 動物實驗 | Animal Models | PC-3M, BT474, BxPc3, LoVo, U87MG, H125 和H460細胞皮下注射到無胸腺雌性小鼠右側 |
| Dosages | ≤100 mg/kg | |
| Administration | 口服處理 | |
| 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 |
|
化學信息&溶解度
| 分子量 | 665.66 | 分子式 | C21H20F3N7O3S.C6H6O3S |
| CAS號 | 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 | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
4-Methylpyridine : 25 mg/mL (37.55 mM) DMSO : 0.4 mg/mL ( (0.6 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble |
摩爾濃度計算器 |
|
體內溶解配方 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內配方計算器 | |||||
實驗計算
動物體內配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
技術支持
在訂購、運輸、儲存和使用我們的產(chǎn)品的任何階段，您遇到的任何問題，均可以通過撥打我們的熱線電話400-668-6834，或者技術支持郵箱[email protected]，直接聯(lián)系到我們。我們會在24小時內盡快聯(lián)系您。
如果有其他問題，請給我們留言。
* 必填項
常見問題及建議解決方法
問題 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.
問題 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.
