Home>>Signaling Pathways>> TGF-β / Smad Signaling>> Pyk2>>PF-562271

PF-562271 Sale

(Synonyms: N-甲基-N-[3-[[[2-[(2-氧代-2,3-二氢-1H-吲哚-5-基)氨基]-5-三氟甲基嘧啶-4-基]氨基]甲基]吡啶-2-基]甲磺酰胺,PF562271;PF 562271) 目录号 : GC15380

A selective FAK/PYK2 inhibitor

PF-562271 Chemical Structure

Cas No.:717907-75-0

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥935.00
现货
5mg
¥861.00
现货
10mg
¥1,439.00
现货
50mg
¥3,392.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Kinase experiment [1]:

Recombinant kinase assay

Purified-activated FAK kinase domain (amino acid 410 ~ 689) was reacted with 50 μmol/L ATP and 10 μg p(Glu/Tyr), in kinase buffer [50 mmol/L HEPES (pH 7.5), 125 mmol/L NaCl and 48 mmol/L MgCl2] for 15 mins. Phosphorylation of p(Glu/Tyr) was challenged with serially diluted PF-562271 at 1/2-Log concentrations starting at a top concentration of 1 μmol/L. Each concentration was tested in triplicate. Phosphorylation of p(Glu/Tyr) was detected with a general antiphospho-tyrosine (PY20) antibody followed by horseradish peroxidase (HRP)-conjugated goat antimouse IgG antibody. HRP substrate was added, and absorbance readings at 450 nm were obtained after addition of stop solution (2 mol/L H2SO4). IC50 values were determined using the Hill-Slope Model.

Cell experiment [1]:

Cell lines

PC3-M cells

Preparation method

The solubility of this compound in DMSO is > 25.4 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

1.1 or 3.3 μmol/L; 48 hrs

Applications

After 48-hour exposure, PF-562271 at the concentration of 3.3 μM altered the cell cycle progression of PC3-M cells. However, the inhibitory activity of PF-562271 against cdk5/p35 enzyme was undetected.

Animal experiment [1]:

Animal models

Nude mice bearing U87MG human glioblastoma cells

Dosage form

3.3, 10 or 33 mg/kg; p.o.

Applications

In nude mice bearing U87MG human glioblastoma cells, PF-562271 inhibited FAK phosphorylation in a dose- and time-dependent manner. After 1-hr exposure to 33 mg/kg PF-562271, maximal pFAK inhibition (78%) was achieved. However, inhibition effect of PF-562271 on FAK phosphorylation was sustained (> 50%) for > 4 hrs after this single p.o. dose. The calculated EC50 value was 93 ng/mL.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Roberts WG, Ung E, Whalen P, Cooper B, Hulford C, Autry C, Richter D, Emerson E, Lin J, Kath J, Coleman K, Yao L, Martinez-Alsina L, Lorenzen M, Berliner M, Luzzio M, Patel N, Schmitt E, LaGreca S, Jani J, Wessel M, Marr E, Griffor M, Vajdos F. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res. 2008 Mar 15;68(6):1935-44. doi: 10.1158/0008-5472.CAN-07-5155.

产品描述

PF-562271 is a potent, ATP-competitive and reversible inhibitor of both focal adhesion kinase (FAK), a non-receptor tyrosine kinase involved in a variety of cellular events, and proline-rich tyrosine kinase 2 (Pyk2), an FAK homolog containing 48% amino acid identity, with half maximal inhibitory concentration (IC50) of 1.5 nmol/L and 14 nmol/L respectively. As a potential therapeutic agent either alone or in combination with other agents for the treatment of cancer, PF-562271 has been reported to effectively inhibit the proliferation of tumors in both xenograft and transgenic mouse models, in which it dose-dependently inhibits FAK phosphorylation in tumor-bearing mice with half maximal effective concentration (EC50) of 93 ng/mL.

References:
[1]Stokes JB, Adair SJ, Slack-Davis JK, Walters DM, Tilghman RW, Hershey ED, Lowrey B, Thomas KS, Bouton AH, Hwang RF, Stelow EB, Parsons JT, Bauer TW. Inhibition of focal adhesion kinase by PF-562,271 inhibits the growth and metastasis of pancreatic cancer concomitant with altering the tumor microenvironment. Mol Cancer Ther. 2011 Nov;10(11):2135-45. doi: 10.1158/1535-7163.MCT-11-0261. Epub 2011 Sep 8.
[2]Roberts WG, Ung E, Whalen P, Cooper B, Hulford C, Autry C, Richter D, Emerson E, Lin J, Kath J, Coleman K, Yao L, Martinez-Alsina L, Lorenzen M, Berliner M, Luzzio M, Patel N, Schmitt E, LaGreca S, Jani J, Wessel M, Marr E, Griffor M, Vajdos F. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res. 2008 Mar 15;68(6):1935-44. doi: 10.1158/0008-5472.CAN-07-5155.

Chemical Properties

Cas No. 717907-75-0 SDF
别名 N-甲基-N-[3-[[[2-[(2-氧代-2,3-二氢-1H-吲哚-5-基)氨基]-5-三氟甲基嘧啶-4-基]氨基]甲基]吡啶-2-基]甲磺酰胺,PF562271;PF 562271
化学名 N-methyl-N-[3-[[[2-[(2-oxo-1,3-dihydroindol-5-yl)amino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]methyl]pyridin-2-yl]methanesulfonamide
Canonical 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
分子式 C21H20F3N7O3S 分子量 507.49
溶解度 ≥ 25.35mg/mL in DMSO, ≥ 2.25 mg/mL in EtOH with ultrasonic and warming 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 1.9705 mL 9.8524 mL 19.7048 mL
5 mM 0.3941 mL 1.9705 mL 3.941 mL
10 mM 0.197 mL 0.9852 mL 1.9705 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置