PF-562271 (Synonyms: PF562271;PF 562271) |
| رقم الكتالوجGC15380 |
PF-562271 (VS-6062) هو مثبط FAK و Pyk2 كيناز قوي ، منافس ATP وقابل للانعكاس مع IC50s من 1.5 نانومتر و 13 نانومتر ، على التوالي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 717907-75-0
Sample solution is provided at 25 µL, 10mM.
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PF-562271 is a potent small-molecule inhibitor of focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (Pyk2) with a IC50 of 1.5 and 14nmol/L, respectively[1][2]. PF-562271 is commonly utilized in the research of various cancers, including pancreatic cancer[3], osteosarcoma and glioblastoma[4], for its potential to inhibit tumor growth and metastasis.
PF-562271 (5µM; 48h) treatment can induce apoptosis and downregulated the activity of the protein kinase B/mammalian target of rapamycin pathway in human osteosarcoma cell lines[5]. PF-562271 (16nM; 72h) treatment combined with 100µM temozolomide (TMZ) signifcantly reduces viability, cell cycle progression, invasion and invadopodia in primary human glioma cell lines[6].
PF-562271(50mg/kg) combined with TMZ enhances the effect of TMZ on tumor growth inhibition and invasiveness in C57Bl/6-GL261 mouse glioma implantation model[6]. When administered orally at a dose of 5mg/kg, PF-562271 suppressed the growth and local spread of intratibial tumors and restored tumor-induced bone loss in nude rats with MDA-MB-231 cells implanted in their tibia[7].
References:
[1]. Michael Luzzio, Christopher Autry, Martin Berliner, et al. Design, synthesis, activity and properties of selective focal adhesion kinase inhibitors which are suitable for advanced preclinical evaluation: The discovery of PF-562271. Cancer Res 1 May 2007; 67 (9_Supplement): 5432.
[2]. Roberts WG, Ung E, Whalen P, et al. 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. PMID: 18339875.
[3]. Stokes JB, Adair SJ, Slack-Davis JK, et al. 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. PMID: 21903606; PMCID: PMC3213273.
[4]. Ortiz Rivera J, Velez Crespo G, Inyushin M, et al. 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]. Hu C, Chen X, Wen J, et al. Antitumor effect of focal adhesion kinase inhibitor PF562271 against human osteosarcoma in vitro and in vivo. Cancer Sci. 2017 Jul;108(7):1347-1356. doi: 10.1111/cas.13256. Epub 2017 Jun 8. Erratum in: Cancer Sci. 2018 Nov;109(11):3663-3664. doi: 10.1111/cas.13804. PMID: 28406574; PMCID: PMC5497929.
[6]. Ortiz-Rivera J, Nuñez R, Kucheryavykh Y, et al. 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.
[7]. Bagi CM, Roberts GW, Andresen CJ. Dual focal adhesion kinase/Pyk2 inhibitor has positive effects on bone tumors: implications for bone metastases. Cancer. 2008 May 15;112(10):2313-21. doi: 10.1002/cncr.23429. PMID: 18348298.
| Cell experiment [1]: | |
Cell lines | human glioblastoma CL-2 cells |
Preparation Method | Cells were treated with 16nM PF-562271 and 100µM TMZ for 72h. Then live and dead cells were quantifed based on calcein and ethidium homodimer-1 staining for live and dead cells. |
Reaction Conditions | 16nM; 72h |
Applications | PF-562271 treatment combined with TMZ reduces cell viability in primary glioblastoma human cell lines compared to TMZ monotherapy. |
| Animal experiment [1]: | |
Animal models | C57Bl/6-GL261 mouse glioma implantation model |
Preparation Method | Beginning on the 5th day after tumor implantation, mice received 2weeks of 50mg/kg PF-562271 combined with 50mg/kg TMZ through oral gavage. Then Immunohistochemical evaluation of tumor size was performed to evaluate effect of PF-562271 on tumor growth. |
Dosage form | 50mg/kg/d; 2weeks; oral |
Applications | Combined PF-562271 and TMZ treatment reduces tumor growth in a C57BL/6 GL261 mouse model |
References: | |
| Cas No. | 717907-75-0 | SDF | |
| المرادفات | PF562271;PF 562271 | ||
| Chemical Name | 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 | ||
| Formula | C21H20F3N7O3S | M.Wt | 507.49 |
| الذوبان | ≥ 25.35mg/mL in DMSO, ≥ 2.25 mg/mL in EtOH with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
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Quality Control & SDS
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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