| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| P408325-1ml |
1ml |
现货  |
|
| 英文别名 | PF-00562271 | Methanesulfonamide, N-[3-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]-2-pyridinyl]-N-methyl- |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | PF-562271 |
| 生化机理 | PF-562271 (PF-00562271) 是一种强效、ATP 竞争性、可逆的 FAK 抑制剂，在无细胞实验中的 IC50 为 1.5 nM，对 Pyk2 的抑制作用比 FAK 弱 10 倍左右，对其他蛋白激酶的选择性大于 100 倍，某些 CDK 除外。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 极光激酶 A 抑制剂；FMS 相关受体酪氨酸激酶 3 抑制剂；蛋白酪氨酸激酶 2 抑制剂；蛋白酪氨酸激酶 2 beta 抑制剂 |
| 产品介绍 |
PF-562271是一种有效的，ATP竞争性的，可逆的FAK抑制剂，IC50为1.5 nM，作用于Pyk2比作用于FAK选择性低10倍左右，比作用于其他蛋白激酶（除了一些CDKs）选择性高100倍以上。 Information PF-562271 (PF-00562271) is a potent, ATP-competitive, reversible inhibitor ofFAKwithIC50of 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 someCDKs. PF-562271 binds in the ATP-binding cleft of FAK, forming two of the three “canonical” H-bonds between the inhibitor and main-chain atoms in the kinase hinge region. PF-562271 is potent in an inducible cell-based assay measuring phospho-FAK with IC50 of 5 nM. PF-562271 (3.3 μM) results in G1 arrest of PC3-M cells. PF-562271 (1 nM) blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays. PF-262271 potently blocks blood vessel sprouting without detectable changes in vascular leakage. PF-562271 (250 nM) results in complete inhibition of collective A431 cell invasion into collagen gels. In vivo PF-562271 (< 33 mg/kg p.o.) inhibits FAK phosphorylation in tumors in a dose- and time-dependent manner in U87MG-bearing mice. PF-562271 (50 mg/kg p.o. bid) results in 86% tumor growth inhibition in BxPc3 xenografts mice and 45% tumor growth inhibition in PC3-M xenografts mice. PF-562271 (25 mg/kg, bid) results in 2-fold greater apoptosis in treated tumors in mice bearing H125 lung xenografts. PF-562271 (33 mg/kg, p.o.) inhibits extensive movement of the tumor cells over 24 hours in mice. PF-562271 (33 mg/kg, p.o.) results in altered E-cadherin dynamics in mice, which correlates with reduced E-cadherin–dependent collective cell movement. PF-562271 (25 mg/kg, p.o. bid) results in 62% tumor growth inhibition in PC3M-luc-C6 subcutaneuous local implant xenograft mouse model. PF-562,271 (5 mg/kg, oral) results in significant and similar increases in osteocalcin and cancellous bone parameters and a decrease in tumor growth and signs of bone healing in rats implanted with MDA-MB-231 cells in the tibia. cell lines： Concentrations： Incubation Time： Powder Purity:≥97% |
| ALogP | 2 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric 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 |
| 关联CAS | 717907-75-0 |
| MeSH Entry Terms | N-methyl-N-(3-(((2-((2-oxo-1,3-dihydroindol-5-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)methyl)pyridin-2-yl)methanesulfonamide;PF-562271;PF562271 |
| 分子量 | 507.49 |
| Reaxy-Rn | 12411620 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12411620&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 63 mg/mL (199.57 mM); Ethanol: 63 mg/mL (199.57 mM); Water: Insoluble; |
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