939791-38-5
PF-562271 benzenesulfonate salt
CAS: 939791-38-5
Molecular Formula: C27H26F3N7O6S2
939791-38-5 - Names and Identifiers
939791-38-5 - Physico-chemical Properties
| Molecular Formula | C27H26F3N7O6S2 |
| Molar Mass | 665.6638496 |
| Solubility | Soluble in DMSO |
| Storage Condition | under inert gas (nitrogen or Argon) at 2-8°C |
| Use | PF-562271 Besylate, also known as PF-562,271 and PF-271, is an orally bioavailable small molecule and ATP-competitive focal adhesion kinase (FAK) 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. Note: PF-562271 benzesulfonate is also called PF-562271 besylate. |
| Target | CDK1/CyclinB; CDK2/CyclinE; CDK3/CyclinE; FAK; PYK2; |
| In vitro study | In recombinant enzyme experiments, PF-562271 Besylate selectively inhibited FAK and Pyk2 tyrosine kinase activity with IC50 of 1.5 nM and 14 nM, respectively. In cell experiments, the IC50 value of PF-562271 for FAK is 5 nM, which is more selective than that for other kinase targets. In two-dimensional culture, PF-562271 inhibited FAK WT,FAK −/− and FAK kinase-deficient (KD) cell proliferation with an IC50 of 3.3 μm, 2.08 μm and 2.01 μm, respectively. |
| In vivo study | PF-562271 Besylate inhibits tumor growth in some human subcutaneous xenograft models in a dose-dependent manner and produces maximum tumor suppression at doses of 25 to 50 mg/kg for PC-3M, BT474, bxPc3, and LoVo cells, twice daily, inhibited by 78% to 94% and no weight loss, morbidity or death occurred. PF-562271 according to the dose of 25 mg/kg oral treatment of subcutaneous and bone metastasis PC3M-LUC-5233 transplanted tumor model, significantly reduced tumor progression. |
939791-38-5 - Reference
| Reference Show more | 1: Tien TY, Wu YJ, Su CH, Wang HH, Hsieh CL, Wang BJ, Su Y, Yeh 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. 2020 Dec 24:ATVBAHA120315650. doi: 10.1161/ATVBAHA.120.315650. Epub ahead of print. PMID: 33356390. 2: 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. 3: 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. 4: 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. |
939791-38-5 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.502 ml | 7.511 ml | 15.023 ml |
| 5 mM | 0.3 ml | 1.502 ml | 3.005 ml |
| 10 mM | 0.15 ml | 0.751 ml | 1.502 ml |
| 5 mM | 0.03 ml | 0.15 ml | 0.3 ml |
Last Update：2024-01-02 23:10:35
939791-38-5 - Reference Information
| biological activity | PF-00562271 Besylate (PF-562271) is a PF-562271 benzenesulfonate, an effective, ATP competitive and reversible FAK inhibitor, IC50 is 1.5 nM, the effect on Pyk2 is about 10 times lower than that on FAK, and the selectivity on other protein kinases (except some CDKs) is more than 100 times higher. Phase 1. |
| target | TargetValue FAK (Cell-Free Assay) 1.5 nmpyk2 (Cell-Free Assay) 13 nmcdk2/CyclinE (Cell-Free Assay) 30 nmcdk3/CyclinE (Cell-Free Assay) 47 nmcdk1/CyclinB (Cell-Free Assay) 58 nm |
| Target | Value |
| FAK (Cell-free assay) | 1.5 nM |
| PYK2 (Cell-free assay) | 13 nM |
| CDK2/CyclinE (Cell-free assay) | 30 nM |
| CDK3/CyclinE (Cell-free assay) | 47 nM |
| CDK1/CyclinB (Cell-free assay) | 58 nM |
| in vitro study | in the recombinase experiment, PF-562271 Besylate selectively inhibited FAK and Pyk2 tyrosine kinase activities with IC50 of 1.5 nM and 14 nM respectively. In cell experiments, the IC50 value of PF-562271 acting on FAK is 5 nM, which is more selective than acting on other kinase targets. In two-dimensional culture, cell proliferation was PF-562271 inhibited by FAK WT,FAK −/−, and FAK kinase deficient (KD) with IC50 of 3.3 μM, 2.08 μM, and 2.01 μM, respectively. |
| in vivo study | PF-562271 Besylate acts on some human subcutaneous transplanted tumor models to inhibit tumor growth. this effect is dose-dependent and produces the maximum tumor inhibitory effect. it acts on PC-3M, BT474, BxPc3, and LoVo cells at a dose of 25 to 50 mg/kg twice a day, inhibiting up to 78% to 94% without weight loss, sick or die. PF-562271 Oral treatment of subcutaneous and bone metastasis PC3M-LUC-5233 transplanted tumor model at a dose of 25 mg/kg significantly reduced tumor progression. |
Last Update：2024-04-10 22:29:15
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