WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H463240
CAS#: 939791-39-6 (mesylate)
Description: PF-562271, also known as VS-6062; PF-562,271, PF-271, is an orally bioavailable FAK inhibitor and The PYK2 inhibitor with potential antineoplastic and antiangiogenic activities. PF-562271 inhibits the tyrosine kinase FAK, and to a lesser extent, proline-rich tyrosine kinase (PYK2), which may inhibit tumor cell migration, proliferation, and survival.
Hodoodo Cat#: H463240
Name: PF-562271 mesylate
CAS#: 939791-39-6 (mesylate)
Chemical Formula: C22H24F3N7O6S2
Exact Mass: 507.13
Molecular Weight: 603.592
Elemental Analysis: C, 43.78; H, 4.01; F, 9.44; N, 16.24; O, 15.90; S, 10.62
This product is not in stock, which may be available by custom synthesis.
For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge).
Quote less than 1g will not be provided. To request quote, please email to sales @hodoodo.com or click below button.
Note: Price will be listed if it is available in the future.
Related CAS #: 939791-38-5 (besylate) 717907-75-0 (free base) 939791-39-6 (mesylate) 939791-41-0 (HCl) 939791-40-9 (tosylate)
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
Appearance: Solid powder
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
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
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 |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: 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.
2: 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.
3: 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.
4: 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.
5: 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.
6: 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.
7: 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.
8: 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.
9: 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.
10: 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.
11: 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.
12: 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.
13: Wang S, Hwang EE, Guha R, O'Neill AF, Melong N, Veinotte CJ, Conway Saur A, Wuerthele K, Shen M, McKnight C, Alexe G, Lemieux ME, Wang A, Hughes E, Xu X, Boxer MB, Hall MD, Kung A, Berman JN, Davis MI, Stegmaier K, Crompton BD. High- throughput Chemical Screening Identifies Focal Adhesion Kinase and Aurora Kinase B Inhibition as a Synergistic Treatment Combination in Ewing Sarcoma. Clin Cancer Res. 2019 Jul 15;25(14):4552-4566. doi: 10.1158/1078-0432.CCR-17-0375. Epub 2019 Apr 12. PMID: 30979745; PMCID: PMC6634997.
14: Chi Q, Wang L, Xie D, Wang X. Characterization of in vitro metabolism of focal adhesion kinase inhibitors by LC/MS/MS. J Pharm Biomed Anal. 2019 May 10;168:163-173. doi: 10.1016/j.jpba.2019.02.028. Epub 2019 Feb 19. PMID: 30807921.
15: Xiang M, Luo H, Wu J, Ren L, Ding X, Wu C, Chen J, Chen S, Zhang H, Yu L, Zou Y, Xu H, Ye P, Chen M, Xia J. ADAM23 in Cardiomyocyte Inhibits Cardiac Hypertrophy by Targeting FAK - AKT Signaling. J Am Heart Assoc. 2018 Sep 18;7(18):e008604. doi: 10.1161/JAHA.118.008604. PMID: 30371220; PMCID: PMC6222933.
16: Wang Y, Zheng J, Han Y, Zhang Y, Su L, Hu D, Fu X. JAM-A knockdown accelerates the proliferation and migration of human keratinocytes, and improves wound healing in rats via FAK/Erk signaling. Cell Death Dis. 2018 Aug 28;9(9):848. doi: 10.1038/s41419-018-0941-y. PMID: 30154481; PMCID: PMC6113279.
17: Liu NG, Yu JN, Hu B, Guo Y, Guo CQ. [Phosphorylated Focal Adhesion Kinase, Phosphinositides 3 Kinase and Aggrecan Genes and Proteins in Cartilage Cells Are Probably Involved in Needle Knife Intervention Induced Improvement of Knee Osteoarthritis in Rabbits]. Zhen Ci Yan Jiu. 2018 Apr 25;43(4):221-5. Chinese. doi: 10.13702/j.1000-0607.170890. PMID: 29888574.
18: Fang Y, Wang D, Xu X, Dava G, Liu J, Li X, Xue Q, Wang H, Zhang J, Zhang H. Preparation, in vitro and in vivo evaluation, and molecular dynamics (MD) simulation studies of novel F-18 labeled tumor imaging agents targeting focal adhesion kinase (FAK). RSC Adv. 2018 Mar 14;8(19):10333-10345. doi: 10.1039/c8ra00652k. PMID: 35540451; PMCID: PMC9078890.
19: Ali D, Abuelreich S, Alkeraishan N, Shwish NB, Hamam R, Kassem M, Alfayez M, Aldahmash A, Alajez NM. Multiple intracellular signaling pathways orchestrate adipocytic differentiation of human bone marrow stromal stem cells. Biosci Rep. 2018 Jan 30;38(1):BSR20171252. doi: 10.1042/BSR20171252. PMID: 29298881; PMCID: PMC5789155.
20: Mazzu YZ, Hu Y, Soni RK, Mojica KM, Qin LX, Agius P, Waxman ZM, Mihailovic A, Socci ND, Hendrickson RC, Tuschl T, Singer S. miR-193b-Regulated Signaling Networks Serve as Tumor Suppressors in Liposarcoma and Promote Adipogenesis in Adipose-Derived Stem Cells. Cancer Res. 2017 Nov 1;77(21):5728-5740. doi: 10.1158/0008-5472.CAN-16-2253. Epub 2017 Sep 7. PMID: 28882999.
