PF-00562271
(Synonyms: PF-562271;PF00562271;PF62271) 目录号 : GC14767
A selective FAK/PYK2 inhibitor
Cas No.:939791-38-5
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
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Cell lines |
Squamous carcinoma cells |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
1 μM, 48 hr |
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Applications |
In squamous carcinoma cells, treatment of the FAK wt expressing cells with the FAK kinase inhibitor PF-562,271 resulted in a similar reduction in cell migration as seen in the FAK-/- cells. PF-562,271 dose-dependently inhibited FAK autophosphorylation on Y397. Treatment with PF-562,271 inhibited golgi orientation. PF-562,271 inhibited Pyk2 and Pyk2 autophosphorylation in PF-562,271 treated cells. Treatment of FAK wt cells with PF-562,271 dose-dependently inhibited cell proliferation. Treatment of FAK wt cells with PF-562,271 (0.25 μM) also resulted in a dose-dependent inhibition of colony formation. Treatment of cells with PF-562,271 in methylcellulose resulted in a small but significant reduction in the number of cells in S phase while the corresponding increase in G1 was not significant. |
| Animal experiment [2,3]: | |
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Animal models |
Mice bearing PC-3M, BT474, BxPc3, and LoVo tumors, |
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Dosage form |
Oral gavage, 25 to 50 mg/kg, twice daily |
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Application |
In several human s.c. xenograft models, PF-562271 dose-dependently inhibited tumor growth, and produced 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. PF-562271 (25 mg/kg by p.o.) significantly decreased tumor progression in both subcutaneous and bone metastasis PC3M-luc-C6 xenograft models. |
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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. |
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References: [1]. Serrels A, McLeod K, Canel M, et al. The role of focal adhesion kinase catalytic activity on the proliferation and migration of squamous cell carcinoma cells[J]. International journal of cancer, 2012, 131(2): 287-297. [2]. Roberts W G, Ung E, Whalen P, et al. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271[J]. Cancer research, 2008, 68(6): 1935-1944. [3]. Roberts W G, Ung E, Whalen P, et al. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271[J]. Cancer research, 2008, 68(6): 1935-1944. | |
| Cas No. | 939791-38-5 | SDF | |
| 别名 | PF-562271;PF00562271;PF62271 | ||
| 化学名 | benzenesulfonic acid;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.C1=CC=C(C=C1)S(=O)(=O)O | ||
| 分子式 | C21H20F3N7O3S.C6H6O3S | 分子量 | 665.66 |
| 溶解度 | ≥ 11.1mg/mL in DMSO with gentle 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。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5023 mL | 7.5113 mL | 15.0227 mL |
| 5 mM | 0.3005 mL | 1.5023 mL | 3.0045 mL |
| 10 mM | 0.1502 mL | 0.7511 mL | 1.5023 mL |
| 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 | 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GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet