PF-562271 Besylate

別名：PF-00562271 Besylate

製品コード：S2672 純度：99.32%

PF-562271 Besylate is the benzenesulfonate salt of PF-562271, which 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. Phase 1.

CAS No. 939791-38-5

サイズ	価格(税別)	在庫状況
5mg	JPY 25500	国内在庫あり
10mg	JPY 40500	国内在庫あり
50mg	JPY 122500	国内在庫あり
1g	JPY 598500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（26）

カスタマーフィードバック4例

製品安全説明書

現在のバッチを見る：純度： 99.32%

99.32

PF-562271 Besylate関連製品

関連製品	PF-562271 PF-573228 Defactinib (VS-6063) VS-4718 (PND-1186) PF-562271 HCl TAE226 (NVP-TAE226) GSK2256098 PF-431396 Y15	もっと見る
関連化合物ライブラリー	Tyrosine Kinase Inhibitor Library PI3K/Akt Inhibitor Library Angiogenesis Related compound Library HIF-1 Signaling Pathway Compound Library FDA-approved Anticancer Drug Library	もっと見る

シグナル伝達経路

FAKシグナル伝達経路

FAK阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	活性情報	PMID
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
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Targets

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)	もっとクリックする
1.5 nM	13 nM	30 nM	47 nM	58 nM	もっとクリックする

In Vitro
In vitro	PF-562271 Besylate 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]
Kinase Assay	Recombinant kinase assay and enzyme kinetics
Kinase Assay	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.
細胞実験	細胞株	Squamous cell carcinoma (SCC)
	濃度	0 to 1 μM
	反応時間	72 hours
	実験の流れ	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.

In Vivo
In Vivo	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]
動物実験	動物モデル	PC-3M, BT474, BxPc3, LoVo, U87MG, H125 and H460 cells are injected s.c. into the right flank of athymic female mice .
	投与量	≤100 mg/kg
	投与経路	Administered via p.o.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (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

参考
[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

参考

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

+ 展開

化学情報

分子量	665.66	化学式	C₂₁H₂₀F₃N₇O₃S.C₆H₆O₃S
CAS No.	939791-38-5	SDF	Download PF-562271 Besylate SDFをダウンロードする
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
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

4-Methylpyridine : 25 mg/mL

DMSO : 0.4 mg/mL ( (0.6 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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よくある質問（FAQ）

質問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.

質問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):