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PF-431396
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PF-431396图片
CAS NO:717906-29-1
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)506.5
FormulaC22H21F3N6O3S
CAS No.717906-29-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (197.43 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Other infoChemical Name: N-Methyl-N-[2-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide
InChi Key: POJZIZBONPAWIV-UHFFFAOYSA-N
InChi Code: InChI=1S/C22H21F3N6O3S/c1-31(35(2,33)34)18-6-4-3-5-13(18)11-26-20-16(22(23,24)25)12-27-21(30-20)28-15-7-8-17-14(9-15)10-19(32)29-17/h3-9,12H,10-11H2,1-2H3,(H,29,32)(H2,26,27,28,30)
SMILES Code: CS(=O)(N(C)C1=CC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O
SynonymsPF 431396; PF431396; PF-431396;
实验参考方法
In Vitro

In vitro activity: In A20 cells, PF-431396 blocks anti-Ig- and clustering LFA-1-induced tyrosine phosphorylation of Pyk2 and FAK, and further blocks B cell spreading. PF-431396 consistently inhibits the increase in protein tyrosine phosphorylation (PY) induced by the absence of added calcium and induced by W-7 in the presence of calcium.


Kinase Assay: PF-431396 is dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor (IC50 values are 2 and 11 nM respectively), PF-431396 has a Kd value of 445 nM for BRD4. IC50 value: 2 nM (FAK); 11 nM (PYK2); 445 nM (KD for BRD4) [1] [2] Target: FAK; PYK2; BRD4 in vitro: PF-431396 is a potent and highly selective pyrimidine-based inhibitor of both Pyk2 and FAK, Consistent with the idea that the tyrosine phosphorylation of Pyk2 and FAK involves an initial autophosphorylation or transphosphorylation step, treating A20 cells with PF-431396 blocked anti-Ig-induced tyrosine phosphorylation of Pyk2 and FAK when the cells were stimulated in suspension when they were stimulated on ECM. Nanomolar affinities were also determined for PF-431396 (Kd = 445 ± 42 nM) and for the PIM inhibitor (Kd = 565 ± 63 nM).

In Vivo
Animal model
Formulation & Dosage
ReferencesJ Biol Chem. 2009 May 8;284(19):13193-201; J Biol Chem. 2009 Aug 21;284(34):22865-77.
生物活性


PF-4618433 promotes osteogenesis of hMSC cultures. hMSC cultures were treated with PF-431396 (days 4-7) or with PF-4618433 (days 1-7), and alkaline phosphatase activity determined on day 7 (A and B, respectively). J Biol Chem. 2009 May 8;284(19):13193-201.



SPR analysis of PYK2 compound binding kinetics. J Biol Chem. 2009 May 8;284(19):13193-201.


A, molecular surface of the PYK2 in the active site region in complex with ATPγS (magenta). Critical side chains are labeled (ball and stick representation) with hydrogen bonds (dashed lines). B, active site of PYK2 bound to PF-431396 (magenta). Hydrophobic residues interacting with the sulfonamide group are shown in yellow. J Biol Chem. 2009 May 8;284(19):13193-201.