PF562271 hydrochloride. PF271, PF-271, PF 271
N-methyl-N-(3-(((2-((2-oxoindolin-5-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)methyl)pyridin-2-yl)methanesulfonamide hydrochloride
CAS: 939791-41-0
Molecular Formula: C21H21ClF3N7O3S
PF562271 hydrochloride. PF271, PF-271, PF 271 - Names and Identifiers
PF562271 hydrochloride. PF271, PF-271, PF 271 - Physico-chemical Properties
| Molecular Formula | C21H21ClF3N7O3S |
| Molar Mass | 543.95 |
| Solubility | Soluble in DMSO |
| Storage Condition | -20℃ |
| Use | PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. |
| Target | IC50: 1.5 nM (FAK), 13 nM (Pyk2), 30 nM (CDK2), 47 nM (CDK3), 58 nM (CDK1), 97 nM (CDK7), 97 nM (Flt3) |
| In vitro study | PF-562271 binding to the ATP-binding site of FAK forms two of the three "standard" hydrogen atoms between the inhibitor and the backbone atom in the kinase hinge region. PF-562271 was effective in the inducible cellular level assay with an IC50 of 5 nM for the determination of phospho-FAK. PF-562271 (3.3 μm) caused a G1 phase arrest in PC3-M cells. PF-562271 (1 nM) blocked bFGF-stimulated revascularization in a chick embryo chorioallantoic membrane assay. PF-262271 potently blocked vascular proliferation with no detectable change in vascular leakage. PF-562271 (250 nM) completely inhibited the invasion of all A431 cells into collagen gel. |
| In vivo study | PF-562271 (< 33 mg/kg p.o.) dose-time dependently inhibited FAK phosphorylation in tumors in U87MG mice. PF-562271 (50 mg/kg p.o. bid) caused 86% tumor growth inhibition in BxPc3 xenograft mice PC3-M 45% tumor growth inhibition in xenograft mice. PF-562271 (25 mg/kg, bid) induced twice as much apoptosis in xenografted H125 lung cancer treated tumors in mice. PF-562271 (33 mg/kg, p.o.) was able to inhibit the extensive movement of tumor cells in mice for more than 24 hours. PF-562271 (33 mg/kg, p.o.) resulted in altered E-cadherin kinetics in mice, which was associated with reduced E-cadherin-dependent collective cell movement. In a PC3M-luc-C6 subcutaneous local xenograft mouse model, PF-562271 (25 mg/kg, p.o. bid) caused a 62% inhibition of tumor growth. In rat tibiae implanted with MDA-MB-231 cells, PF-562,271 (5 mg/kg, oral) caused a significant and similar increase in osteocalcin and cancellous bone parameters, a decrease in tumor growth, and the emergence of bone healing signals. |
PF562271 hydrochloride. PF271, PF-271, PF 271 - 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. 5: 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: 10.10 |
PF562271 hydrochloride. PF271, PF-271, PF 271 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.838 ml | 9.192 ml | 18.384 ml |
| 5 mM | 0.368 ml | 1.838 ml | 3.677 ml |
| 10 mM | 0.184 ml | 0.919 ml | 1.838 ml |
| 5 mM | 0.037 ml | 0.184 ml | 0.368 ml |
Last Update：2024-01-02 23:10:35
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Product Name: N-methyl-N-(3-(((2-((2-oxoindolin-5-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)methyl)pyridin-2-yl)methanesulfonamide hydrochloride Visit Supplier Webpage Request for quotationCAS: 939791-41-0
Tel: 18301782025
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Mobile: 18021002903
QQ: 3008007409
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