PF-562271 Besylate

別名: PF-00562271 Besylate

目錄號：S2672 Purity: 99.32%

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

規(guī)格	價格	庫存
5mg	1392.3	現(xiàn)貨
10mg	2211.3	現(xiàn)貨
50mg	6691.23	現(xiàn)貨
200mg	16298.1	現(xiàn)貨
1g	31900	現(xiàn)貨
更大包裝有超大折扣
400-668-6834 info@selleck.cn

產(chǎn)品質(zhì)控

批次：純度： 99.32%

99.32

PF-562271 Besylate相關(guān)產(chǎn)品

相關(guān)產(chǎn)品	PF-562271 PF-573228 Defactinib (VS-6063) VS-4718 (PND-1186) PF-562271 HCl TAE226 (NVP-TAE226) GSK2256098 PF-431396 Y15	點(diǎn)擊展開
相關(guān)化合物庫	酪氨酸激酶抑制劑分子庫 PI3K/Akt 抑制劑庫血管生成相關(guān)化合物庫 HIF-1信號通路化合物庫 FDA抗癌藥物庫	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	活性描述	文獻(xiàn)信息
human SNU-387 cell	Growth inhibition assay	Inhibition of human SNU-387 cell growth in a cell viability assay, IC50=2.5282 μM	SANGER
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	SANGER
human DU-145 cell	Growth inhibition assay	Inhibition of human DU-145 cell growth in a cell viability assay, IC50=2.49118 μM	SANGER
human MFE-296 cell	Growth inhibition assay	Inhibition of human MFE-296 cell growth in a cell viability assay, IC50=2.47792 μM	SANGER
human DU-4475 cell	Growth inhibition assay	Inhibition of human DU-4475 cell growth in a cell viability assay, IC50=2.14759 μM	SANGER
human NCI-H460 cell	Growth inhibition assay	Inhibition of human NCI-H460 cell growth in a cell viability assay, IC50=2.04839 μM	SANGER
human U251 cell	Growth inhibition assay	Inhibition of human U251 cell growth in a cell viability assay, IC50=1.74031 μM	SANGER
human EW-13 cell	Growth inhibition assay	Inhibition of human EW-13 cell growth in a cell viability assay, IC50=1.63466 μM	SANGER
human SW1710 cell	Growth inhibition assay	Inhibition of human SW1710 cell growth in a cell viability assay, IC50=1.62628 μM	SANGER
human MZ1-PC cell	Growth inhibition assay	Inhibition of human MZ1-PC cell growth in a cell viability assay, IC50=1.62312 μM	SANGER
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	SANGER
human BC-1 cell	Growth inhibition assay	Inhibition of human BC-1 cell growth in a cell viability assay, IC50=1.61664 μM	SANGER
human HSC-2 cell	Growth inhibition assay	Inhibition of human HSC-2 cell growth in a cell viability assay, IC50=1.5395 μM	SANGER
human ST486 cell	Growth inhibition assay	Inhibition of human ST486 cell growth in a cell viability assay, IC50=1.53278 μM	SANGER
human AGS cell	Growth inhibition assay	Inhibition of human AGS cell growth in a cell viability assay, IC50=1.52124 μM	SANGER
human SIG-M5 cell	Growth inhibition assay	Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=1.48487 μM	SANGER
human HUTU-80 cell	Growth inhibition assay	Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=1.44886 μM	SANGER
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	SANGER
human KYSE-150 cell	Growth inhibition assay	Inhibition of human KYSE-150 cell growth in a cell viability assay, IC50=1.35236 μM	SANGER
human CAL-62 cell	Growth inhibition assay	Inhibition of human CAL-62 cell growth in a cell viability assay, IC50=1.31909 μM	SANGER
human MES-SA cell	Growth inhibition assay	Inhibition of human MES-SA cell growth in a cell viability assay, IC50=1.30682 μM	SANGER
human BPH-1 cell	Growth inhibition assay	Inhibition of human BPH-1 cell growth in a cell viability assay, IC50=1.28766 μM	SANGER
human NKM-1 cell	Growth inhibition assay	Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=1.27506 μM	SANGER
human AN3-CA cell	Growth inhibition assay	Inhibition of human AN3-CA cell growth in a cell viability assay, IC50=1.21867 μM	SANGER
human CAL-33 cell	Growth inhibition assay	Inhibition of human CAL-33 cell growth in a cell viability assay, IC50=1.12938 μM	SANGER
NCI-H810 cell	Growth inhibition assay	Inhibition of human NCI-H810 cell growth in a cell viability assay, IC50=1.10776 μM	SANGER
human 8305C cell	Growth inhibition assay	Inhibition of human 8305C cell growth in a cell viability assay, IC50=1.09904 μM	SANGER
human KYSE-270 cell	Growth inhibition assay	Inhibition of human KYSE-270 cell growth in a cell viability assay, IC50=1.04714 μM	SANGER
ALL-PO cell	Growth inhibition assay	Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=1.01584 μM	SANGER
human BCPAP cell	Growth inhibition assay	Inhibition of human BCPAP cell growth in a cell viability assay, IC50=1.01288 μM	SANGER
human RT-112 cell	Growth inhibition assay	Inhibition of human RT-112 cell growth in a cell viability assay, IC50=0.9846 μM	SANGER
human NCI-H650 cell	Growth inhibition assay	Inhibition of human NCI-H650 cell growth in a cell viability assay, IC50=0.83154 μM	SANGER
human IGROV-1 cell	Growth inhibition assay	Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=0.81038 μM	SANGER
human MG-63 cell	Growth inhibition assay	Inhibition of human MG-63 cell growth in a cell viability assay, IC50=0.80637 μM	SANGER
human COLO-829 cell	Growth inhibition assay	Inhibition of human COLO-829 cell growth in a cell viability assay, IC50=0.76176 μM	SANGER
human COLO-205 cell	Growth inhibition assay	Inhibition of human COLO-205 cell growth in a cell viability assay, IC50=0.48658 μM	SANGER
human KM12 cell	Growth inhibition assay	Inhibition of human KM12 cell growth in a cell viability assay, IC50=0.38557 μM	SANGER
human SW982 cell	Growth inhibition assay	Inhibition of human SW982 cell growth in a cell viability assay, IC50=0.3282 μM	SANGER
MV-4-11 cell	Growth inhibition assay	Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=0.2766 μM	SANGER
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點(diǎn)

FAK ^[1] (Cell-free assay)	PYK2 ^[1] (Cell-free assay)	CDK2/CyclinE ^[1] (Cell-free assay)	CDK3/CyclinE ^[1] (Cell-free assay)	CDK1/CyclinB ^[1] (Cell-free assay)	點(diǎn)擊更多
1.5 nM	13 nM	30 nM	47 nM	58 nM	點(diǎn)擊更多

體外研究(In Vitro)
體外研究活性	在重組酶實(shí)驗(yàn)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(xì)胞實(shí)驗(yàn)中，PF-562271 作用于FAK的IC50值為5 nM，比作用于其他激酶靶點(diǎn)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(xì)胞增殖，IC50分別為3.3 μM, 2.08 μM 和 2.01 μM。^[2]
激酶實(shí)驗(yàn)	重組激酶實(shí)驗(yàn)和酶動力學(xué)
激酶實(shí)驗(yàn)	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(jī)肽聚合物,在激酶buffer [50 mM HEPES (pH 7.5), 125 mM NaCl, 和 48 mM MgCl₂] 中反應(yīng)15分鐘。使用從1 μM連續(xù)稀釋的PF-562271 進(jìn)行p(Glu/Tyr)磷酸化。實(shí)驗(yàn)中每種實(shí)驗(yàn)濃度重復(fù)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(biāo)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(wù)系統(tǒng)通過UpState生物技術(shù)進(jìn)行廣譜激酶選擇譜研究。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	鱗狀細(xì)胞癌(SCC)
	濃度	0 到1 μM
	孵育時間	72小時
	方法	細(xì)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(xì)胞，3天后，使用 Sulforhodamine B(SRB) 染料染色。使用1% 冰醋酸沖洗實(shí)驗(yàn)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(fù)測定中獲得IC50值。

體內(nèi)研究(In Vivo)
體內(nèi)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(xì)胞，每天兩次，抑制達(dá)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(zhuǎn)移PC3M-LUC-5233移植瘤模型，顯著降低腫瘤進(jìn)展。^[3]
動物實(shí)驗(yàn)	Animal Models	PC-3M, BT474, BxPc3, LoVo, U87MG, H125 和H460細(xì)胞皮下注射到無胸腺雌性小鼠右側(cè)
	Dosages	≤100 mg/kg
	Administration	口服處理

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT00666926	Completed	Head and Neck Neoplasm\|Prostatic Neoplasm\|Pancreatic Neoplasm	Verastem Inc.	December 2005	Phase 1

參考文獻(xiàn)
[1] Roberts WG, et al. Cancer Res. 2008, 68(6), 1935-1944. [2] Serrels A, et al. Int J Cancer. 2012, 131(2), 287-297. [3] Sun H, et al. Cancer Biol Ther. 2010, 10(1), 38-43. [4] Bagi CM, et al. Cancer Biol Ther. 2009, 8(9), 856-865. + 展開

參考文獻(xiàn)

[1] Roberts WG, et al. Cancer Res. 2008, 68(6), 1935-1944.
[2] Serrels A, et al. Int J Cancer. 2012, 131(2), 287-297.
[3] Sun H, et al. Cancer Biol Ther. 2010, 10(1), 38-43.

[4] Bagi CM, et al. Cancer Biol Ther. 2009, 8(9), 856-865.

+ 展開

化學(xué)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)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

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

DMSO : 100 mg/mL ( (150.22 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

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(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(nèi)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(jì)算結(jié)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(nèi)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(nèi)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(jìn)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(shù)支持

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操作手冊

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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.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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