PF-00562271
N-Methyl-N-[3-[[[2-[(2-oxo-2,3-dihydro-1H-indol-5-yl)amino]-5-trifluoromethylpyrimidin-4-yl]amino]methyl]pyridin-2-yl]methanesulfonamide
CAS: 717907-75-0
Molecular Formula: C21H20F3N7O3S
PF-00562271 - Names and Identifiers
PF-00562271 - Physico-chemical Properties
| Molecular Formula | C21H20F3N7O3S |
| Molar Mass | 507.49 |
| Density | 1.540 |
| Melting Point | >204°C (dec.) |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | White powder. |
| Color | White to Off-White |
| pKa | 13.66±0.20(Predicted) |
| Storage Condition | Hygroscopic, -20°C Freezer, Under inert atmosphere |
| Use | PF-562271 is an effective, ATP competitive and reversible FAK inhibitor. IC50 is 1.5 nM. The selectivity for Pyk2 is about 10 times lower than that for FAK and more than 100 times higher than that for other protein kinases (except some CDKs). |
| In vitro study | PF-562271 will bind to the site where ATP binds to FAK, forming two hydrogen bonds between the inhibitor and the backbone atoms in the kinase hinge region. PF-562271 worked well in cell-based assays measuring inducible FAK phosphorylation with an IC50 of 5 nM. PF-562271 (3.3 μm) caused PC3-M cell cycle arrest in the G1 phase. PF-562271 (1nm) blocked bFGF-stimulated angiogenesis in chick chorioallantoic membrane experiments. PF-262271 strongly and effectively blocked vascular growth but had no significant effect on vascular leakage. PF-562271 (250 nM) completely inhibited the invasion of whole body A431 cells into collagen. |
| In vivo study | PF-562271 (< 33 mg/kg P. O.) inhibited FAK phosphorylation in tumors with a time-and dose-dependent profile in mice carrying U87MG. The tumor growth inhibition rate of PF-562271 (50 mg/kg, oral, twice a day) was 86% in BxPc3 xenograft mice and 45% in PC3-M xenograft mice. PF-562271 (25 mg/kg, twice a day) treatment of h125-bearing lung xenograft tumors increased the rate of apoptosis by 2-fold. PF-562271 (33 mg/kg, P. O.) inhibits widespread motility of tumor cells in mice after 24 hours. PF-562271 (33 mg/kg P. O.) results in altered E-cadherin kinetics in mice, which is associated with reduced E-cadherin-dependent global cell motility. PF-562271 (25 mg/kg P. O., twice a day) resulted in a 62% inhibition of tumor growth in a mouse model of subcutaneous local xenograft PC3M-luc-C6. PF-562271 (5 mg/kg, P. O.) in rats implanted with MDA-MB-231 cells in the tibia resulted in a significant and similar increase in osteocalcin and cancellous bone parameters and a decrease in tumor growth rate and bone healing signal. |
PF-00562271 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.97 ml | 9.852 ml | 19.705 ml |
| 5 mM | 0.394 ml | 1.97 ml | 3.941 ml |
| 10 mM | 0.197 ml | 0.985 ml | 1.97 ml |
| 5 mM | 0.039 ml | 0.197 ml | 0.394 ml |
Last Update：2024-01-02 23:10:35
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Product Name: PF-562271 Visit Supplier Webpage Request for quotationCAS: 717907-75-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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