Synonym
PF-562271 mesylate ; PF562271; PF562271; PF-562271; PF562,271; PF562,271; PF-562,271; PF-00562271; PF00562271; PF 00562271; PF271, PF-271, PF 271; VS-6062; VS-6062; VS 6062;
IUPAC/Chemical Name
N-methyl-N-(3-(((2-((2-oxoindolin-5-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)methyl)pyridin-2-yl)methanesulfonamide mesylate
InChi Key
LMGBAHJMBMDBFE-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H20F3N7O3S.CH4O3S/c1-31(35(2,33)34)19-12(4-3-7-25-19)10-26-18-15(21(22,23)24)11-27-20(30-18)28-14-5-6-16-13(8-14)9-17(32)29-16;1-5(2,3)4/h3-8,11H,9-10H2,1-2H3,(H,29,32)(H2,26,27,28,30);1H3,(H,2,3,4)
SMILES Code
CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O.OS(=O)(C)=O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
603.59
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
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2: He Y, Gang B, Zhang M, Bai Y, Wan Z, Pan J, Liu J, Liu G, Gu W. ACE2 improves endothelial cell function and reduces acute lung injury by downregulating FAK expression. Int Immunopharmacol. 2024 Feb 15;128:111535. doi: 10.1016/j.intimp.2024.111535. Epub 2024 Jan 20. PMID: 38246001.
3: Liu J, Tang L, Chu W, Wei L. Cellular Retinoic Acid Binding Protein 2 (CRABP2), Up-regulated by HPV E6/E7, Leads to Aberrant Activation of the Integrin β1/FAK/ERK Signaling Pathway and Aggravates the Malignant Phenotypes of Cervical Cancer. Biochem Genet. 2023 Nov 24. doi: 10.1007/s10528-023-10568-6. Epub ahead of print. PMID: 38001389.
4: Ortiz Rivera J, Velez Crespo G, Inyushin M, Kucheryavykh Y, Kucheryavykh L. Pyk2/FAK Signaling Is Upregulated in Recurrent Glioblastoma Tumors in a C57BL/6/GL261 Glioma Implantation Model. Int J Mol Sci. 2023 Aug 30;24(17):13467. doi: 10.3390/ijms241713467. PMID: 37686276; PMCID: PMC10487692.
5: Leung PKH, Das B, Cheng X, Tarazi M. Prognostic and Predictive Utility of GPD1L in Human Hepatocellular Carcinoma. Int J Mol Sci. 2023 Aug 23;24(17):13113. doi: 10.3390/ijms241713113. PMID: 37685919; PMCID: PMC10487989.
6: Liu Y, Shen B, Huang T, Wang J, Jiang J. Construction and validation of 3-genes hypoxia-related prognostic signature to predict the prognosis and therapeutic response of hepatocellular carcinoma patients. PLoS One. 2023 Jul 5;18(7):e0288013. doi: 10.1371/journal.pone.0288013. PMID: 37406019; PMCID: PMC10321610.
7: Pan Q, Wang Q, Zhao T, Zhao X, Liang Y, Shi M, Chen C, Lin F. FAK inhibitor PF-562271 inhibits the migration and proliferation of high-grade serous ovarian cancer cells through FAK and FAK mediated cell cycle arrest. Med Oncol. 2023 Jun 29;40(8):215. doi: 10.1007/s12032-023-02092-9. PMID: 37382687.
8: Xu C, Zhang W, Liu C. FAK downregulation suppresses stem-like properties and migration of human colorectal cancer cells. PLoS One. 2023 Apr 21;18(4):e0284871. doi: 10.1371/journal.pone.0284871. PMID: 37083591; PMCID: PMC10121060.
9: Ortiz-Rivera J, Nuñez R, Kucheryavykh Y, Kucheryavykh L. The PYK2 inhibitor PF-562271 enhances the effect of temozolomide on tumor growth in a C57Bl/6-Gl261 mouse glioma model. J Neurooncol. 2023 Feb;161(3):593-604. doi: 10.1007/s11060-023-04260-3. Epub 2023 Feb 15. PMID: 36790653; PMCID: PMC9992029.
10: Yu HJ, Shin JA, Cho SD. Inhibition of focal adhesion kinase/paxillin axis by caffeic acid phenethyl ester restrains aggressive behaviors of head and neck squamous cell carcinoma in vitro. Arch Oral Biol. 2023 Feb;146:105611. doi: 10.1016/j.archoralbio.2022.105611. Epub 2022 Dec 24. PMID: 36577313.
11: Zhao T, Liu B, Zhang M, Li S, Zhao C, Cheng L. Assessment of alterations in histone modification function and guidance for death risk prediction in cervical cancer patients. Front Genet. 2022 Sep 19;13:1013571. doi: 10.3389/fgene.2022.1013571. PMID: 36199574; PMCID: PMC9527294.
12: Qin Q, Wang R, Fu Q, Zhang G, Wu T, Liu N, Lv R, Yin W, Sun Y, Sun Y, Zhao D, Cheng M. Design, synthesis, and biological evaluation of potent FAK-degrading PROTACs. J Enzyme Inhib Med Chem. 2022 Dec;37(1):2241-2255. doi: 10.1080/14756366.2022.2100886. PMID: 35978496; PMCID: PMC9455338.
13: Luo W, Han Y, Li X, Liu Z, Meng P, Wang Y. Breast Cancer Prognosis Prediction and Immune Pathway Molecular Analysis Based on Mitochondria-Related Genes. Genet Res (Camb). 2022 May 31;2022:2249909. doi: 10.1155/2022/2249909. PMID: 35707265; PMCID: PMC9174003.
14: Cho H, Shin I, Yoon H, Jeon E, Lee J, Kim Y, Ryu S, Song C, Kwon NH, Moon Y, Kim S, Kim ND, Choi HG, Sim T. Identification of Thieno[3,2-d]pyrimidine Derivatives as Dual Inhibitors of Focal Adhesion Kinase and FMS-like Tyrosine Kinase 3. J Med Chem. 2021 Aug 26;64(16):11934-11957. doi: 10.1021/acs.jmedchem.1c00459. Epub 2021 Jul 29. PMID: 34324343.
15: Tan H, Liu Y, Gong C, Zhang J, Huang J, Zhang Q. Synthesis and evaluation of FAK inhibitors with a 5-fluoro-7H-pyrrolo[2,3-d]pyrimidine scaffold as anti- hepatocellular carcinoma agents. Eur J Med Chem. 2021 Nov 5;223:113670. doi: 10.1016/j.ejmech.2021.113670. Epub 2021 Jun 25. PMID: 34214842.
16: Tien (田婷怡) TY, Wu (吳懿哲) YJ, Su (蘇正煌) CH, Wang (王學孝) HH, Hsieh (謝金玲) CL, Wang (王博正) BJ, Su (蘇瑀) Y, Yeh (葉宏一) HI. Reduction of Connexin 43 Attenuates Angiogenic Effects of Human Smooth Muscle Progenitor Cells via Inactivation of Akt and NF-κB Pathway. Arterioscler Thromb Vasc Biol. 2021 Feb;41(2):915-930. doi: 10.1161/ATVBAHA.120.315650. Epub 2020 Dec 24. PMID: 33356390.
17: Shi Y, Bray W, Smith AJ, Zhou W, Calaoagan J, Lagisetti C, Sambucetti L, Crews P, Lokey RS, Webb TR. An exon skipping screen identifies antitumor drugs that are potent modulators of pre-mRNA splicing, suggesting new therapeutic applications. PLoS One. 2020 May 29;15(5):e0233672. doi: 10.1371/journal.pone.0233672. PMID: 32469945; PMCID: PMC7259758.
18: Fenelon JC, Xu B, Baltz JM. Focal adhesion kinase PTK2 autophosphorylation is not required for the activation of sodium-hydrogen exchange by decreased cell volume in the preimplantation mouse embryo. Zygote. 2019 Jun;27(3):173-179. doi: 10.1017/S0967199419000212. Epub 2019 Jun 7. PMID: 31171046.
19: Hong KO, Ahn CH, Yang IH, Han JM, Shin JA, Cho SD, Hong SD. Norcantharidin Suppresses YD-15 Cell Invasion Through Inhibition of FAK/Paxillin and F-Actin Reorganization. Molecules. 2019 May 19;24(10):1928. doi: 10.3390/molecules24101928. PMID: 31109130; PMCID: PMC6572169.
20: Al-Ghabkari A, Qasrawi DO, Alshehri M, Narendran A. Focal adhesion kinase (FAK) phosphorylation is a key regulator of embryonal rhabdomyosarcoma (ERMS) cell viability and migration. J Cancer Res Clin Oncol. 2019 Jun;145(6):1461-1469. doi: 10.1007/s00432-019-02913-3. Epub 2019 Apr 21. PMID: 31006845.
1. Murphy JM, Jeong K, Cioffi DL, Campbell PM, Jo H, Ahn EE, Lim SS. Focal Adhesion Kinase Activity and Localization is Critical for TNF-α-Induced Nuclear Factor-κB Activation. Inflammation. 2021 Feb 2. doi: 10.1007/s10753-020-01408-5. Epub ahead of print. PMID: 33527321.
2. Ortiz-Rivera J, Nuñez R, Kucheryavykh Y, Kucheryavykh L. The PYK2 inhibitor PF-562271 enhances the effect of temozolomide on tumor growth in a C57Bl/6-Gl261 mouse glioma model. J Neurooncol. 2023 Feb;161(3):593-604. doi: 10.1007/s11060-023-04260-3. Epub 2023 Feb 15. PMID: 36790653; PMCID: PMC9992029.
3. Rolón-Reyes K, Kucheryavykh YV, Cubano LA, Inyushin M, Skatchkov SN, Eaton MJ, Harrison JK, Kucheryavykh LY. Microglia Activate Migration of Glioma Cells through a Pyk2 Intracellular Pathway. PLoS One. 2015 Jun 22;10(6):e0131059. doi: 10.1371/journal.pone.0131059. PMID: 26098895; PMCID: PMC4476590.
4. Lu H, Wang L, Gao W, Meng J, Dai B, Wu S, Minna J, Roth JA, Hofstetter WL, Swisher SG, Fang B. IGFBP2/FAK pathway is causally associated with dasatinib resistance in non-small cell lung cancer cells. Mol Cancer Ther. 2013 Dec;12(12):2864-73. doi: 10.1158/1535-7163.MCT-13-0233. Epub 2013 Oct 15. PMID: 24130049; PMCID: PMC3858413.
5. Kuonen F, Surbeck I, Sarin KY, Dontenwill M, Rüegg C, Gilliet M, Oro AE, Gaide O. TGFβ, Fibronectin and Integrin α5β1 Promote Invasion in Basal Cell Carcinoma. J Invest Dermatol. 2018 Nov;138(11):2432-2442. doi: 10.1016/j.jid.2018.04.029. Epub 2018 Jul 14. PMID: 29758283; PMCID: PMC6207534.
6. Gao C, Chen G, Kuan SF, Zhang DH, Schlaepfer DD, Hu J. FAK/PYK2 promotes the Wnt/β-catenin pathway and intestinal tumorigenesis by phosphorylating GSK3β. Elife. 2015 Sep 3;4:e10072. doi: 10.7554/eLife.10072. PMID: 26274564; PMCID: PMC4558782.
7. Chen G, Gao C, Gao X, Zhang DH, Kuan SF, Burns TF, Hu J. Wnt/β-Catenin Pathway Activation Mediates Adaptive Resistance to BRAF Inhibition in Colorectal Cancer. Mol Cancer Ther. 2018 Apr;17(4):806-813. doi: 10.1158/1535-7163.MCT-17-0561. Epub 2017 Nov 22. PMID: 29167314; PMCID: PMC5882543.
8. Jeong K, Murphy JM, Rodriguez YAR, Kim JS, Ahn EE, Lim SS. FAK inhibition reduces metastasis of α4 integrin-expressing melanoma to lymph nodes by targeting lymphatic VCAM-1 expression. Biochem Biophys Res Commun. 2019 Feb 19;509(4):1034-1040. doi: 10.1016/j.bbrc.2019.01.050. Epub 2019 Jan 17. PMID: 30660359; PMCID: PMC6350924.
9. Murphy JM, Jeong K, Rodriguez YAR, Kim JH, Ahn EE, Lim SS. FAK and Pyk2 activity promote TNF-α and IL-1β-mediated pro-inflammatory gene expression and vascular inflammation. Sci Rep. 2019 May 20;9(1):7617. doi: 10.1038/s41598-019-44098-2. PMID: 31110200; PMCID: PMC6527705.
10. Kim JS, Lim SS. LED Light-Induced ROS Differentially Regulates Focal Adhesion Kinase Activity in HaCaT Cell Viability. Curr Issues Mol Biol. 2022 Mar 4;44(3):1235-1246. doi: 10.3390/cimb44030082. PMID: 35723305; PMCID: PMC8947587.
11. Lu H, Wang L, Gao W, Meng J, Dai B, Wu S, Minna J, Roth JA, Hofstetter WL, Swisher SG, Fang B. IGFBP2/FAK pathway is causally associated with dasatinib resistance in non-small cell lung cancer cells. Mol Cancer Ther. 2013 Dec;12(12):2864-73. doi: 10.1158/1535-7163.MCT-13-0233. Epub 2013 Oct 15. PMID: 24130049; PMCID: PMC3858413.
12. Knuchel S, Anderle P, Werfelli P, Diamantis E, Rüegg C. Fibroblast surface-associated FGF-2 promotes contact-dependent colorectal cancer cell migration and invasion through FGFR-SRC signaling and integrin αvβ5-mediated adhesion. Oncotarget. 2015 Jun 10;6(16):14300-17. doi: 10.18632/oncotarget.3883. PMID: 25973543; PMCID: PMC4546468.
13. Dahiya S, Saleh M, Rodriguez UA, Rajasundaram D, R Arbujas J, Hajihassani A, Yang K, Sehrawat A, Kalsi R, Yoshida S, Prasadan K, Lickert H, Hu J, Piganelli JD, Gittes GK, Esni F. Acinar to β-like cell conversion through inhibition of focal adhesion kinase. Nat Commun. 2024 May 3;15(1):3740. doi: 10.1038/s41467-024-47972-4. PMID: 38702347; PMCID: PMC11068907.
