- PF-431396
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- $50.00 / 5mg
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2026-03-13
- CAS:717906-29-1
- Min. Order:
- Purity: 99.82%
- Supply Ability: 10g
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| | N-Methyl-N-[2-[[[2-[(2-oxo-2,3-dihydro-1H-indol-5-yl)amino]-5-trifluoromethylpyrimidin-4-yl]amino]methyl]phenyl]methanesulfonamide Basic information |
| | N-Methyl-N-[2-[[[2-[(2-oxo-2,3-dihydro-1H-indol-5-yl)amino]-5-trifluoromethylpyrimidin-4-yl]amino]methyl]phenyl]methanesulfonamide Chemical Properties |
| density | 1.506 | | storage temp. | 2-8°C | | solubility | DMSO: ≥10mg/mL | | form | powder | | pka | 13.66±0.20(Predicted) | | color | off-white to blue-gray | | InChIKey | XSXCARUUZVMRGX-UHFFFAOYSA-N | | SMILES | O.CN(c1ccccc1CNc2nc(Nc3ccc4NC(=O)Cc4c3)ncc2C(F)(F)F)S(C)(=O)=O |
| Hazard Codes | T | | Risk Statements | 25-36 | | Safety Statements | 26-45 | | RIDADR | UN 2811 6.1 / PGIII | | WGK Germany | 3 | | Storage Class | 6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects | | Hazard Classifications | Acute Tox. 3 Oral
Eye Irrit. 2 |
| | N-Methyl-N-[2-[[[2-[(2-oxo-2,3-dihydro-1H-indol-5-yl)amino]-5-trifluoromethylpyrimidin-4-yl]amino]methyl]phenyl]methanesulfonamide Usage And Synthesis |
| Description | Proline-rich tyrosine kinase 2 (PYK2) and focal adhesion kinase (FAK) are nonreceptor tyrosine kinases that constitute the focal adhesion kinase subfamily. PYK2 is expressed in both bone-forming osteoblasts and bone-resorbing osteoclasts where it has a positive role in osteoclast maturation and bone resorption. PF-431396 is a pyrimidine-based dual inhibitor of FAK and PYK2 (IC50s = 2 and 11 nM, respectively). In ovariectomized rats, it has been shown to increase bone formation, promoting osteoblast recruitment and activity. | | Uses | PF 431396 is a dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor (IC50 values are 2 and 11 nM respectively). Promotes osteoblast recruitment and activity, and stimulates bone formation in ovariectomized rats. | | Uses | PF-431396 hydrate has been used as a dual inhibitor of proline-rich tyrosine kinase 2 (PYK2) / focal adhesion kinase (FAK) inhibitor to study its effects on phosphorylation of Yes-associated protein (YAP) at Ser127 and steady state of transcriptional coactivator with PDZ-binding motif (TAZ) . It has also been used as a PYK2/FAK inhibitor to study its effects on protein kinase A activation in human sperm samples . | | Definition | ChEBI: N-methyl-N-[2-[[[2-[(2-oxo-1,3-dihydroindol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide is a sulfonamide. | | Biochem/physiol Actions | PF-431396 is a potent inhibitor of PYK2 and FAK kinases (IC50 = 11 and 1.5 nM, respectively). PF-431396 increases bone formation and protects against bone loss in ovariectomized rats. | | storage | Store at +4°C | | References | [1] SEUNGIL HAN. Structural characterization of proline-rich tyrosine kinase 2 (PYK2) reveals a unique (DFG-out) conformation and enables inhibitor design.[J]. The Journal of Biological Chemistry, 2009, 284 19: 13193-13201. DOI: 10.1074/jbc.m809038200
[2] LEONARD BUCKBINDER. Proline-rich tyrosine kinase 2 regulates osteoprogenitor cells and bone formation, and offers an anabolic treatment approach for osteoporosis.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2007, 104 25: 10619-10624. DOI: 10.1073/pnas.0701421104 |
| | N-Methyl-N-[2-[[[2-[(2-oxo-2,3-dihydro-1H-indol-5-yl)amino]-5-trifluoromethylpyrimidin-4-yl]amino]methyl]phenyl]methanesulfonamide Preparation Products And Raw materials |
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