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PF-573228
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-573228图片
CAS NO:869288-64-2
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
50 mg电议
100 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
PF 573228
产品介绍
PF 573228是一种选择性的FAK抑制剂,对FAK纯化重组催化片段的IC50值为4 nM。

产品描述

PF-573228 is an ATP-competitive FAK inhibitor. In a cell-free assay, the IC50 of FAK is 4 nM.

体内活性

在REF52细胞, PC3细胞, SKOV-3细胞, 及L3.6p1和F-G, MDCK细胞中,PF 573228(IC50=30-500 nM)抑制FAK Tyr397磷酸化。PF 573228(1 μM )抑制FAK磷酸化,但不抑制细胞生长或诱导凋亡。

激酶实验

Affinity determination: Purified activated FAK kinase domain (amino acids 410–689) is reacted with 50 μM ATP, and 10 μg/well of a random peptide polymer of Glu and Tyr (molar ratio of 4:1), poly(Glu/Tyr) in kinase buffer (50 mM HEPES, pH 7.5, 125 mM NaCl, 48 mM MgCl2) for 15 min. Phosphorylation of poly(Glu/Tyr) is challenged with serially diluted compounds at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is run in triplicate. Phosphorylation of poly(Glu/Tyr) is detected with a general anti-phospho-tyrosine (PY20) antibody, followed by horseradish peroxidase-conjugated goat anti-mouse IgG antibody. The standard horseradish peroxidase substrate 3, 3', 5, 5'-tetramethylbenzidine is added, and Optical Density readings at 450 nm are obtained following the addition of stop solution (2 M H2SO4). The IC50 values are determined using the Hill slope model.

细胞实验

Growth assays are performed by seeding 1 × 104 REF52 or PC3 cells/well of a 24-well plate in triplicate 24 h prior to daily treatment with the indicated concentrations of each inhibitor for 3 days. Subsequently, the cells are harvested and counted.(Only for Reference)

Cas No.

869288-64-2

分子式

C22H20F3N5O3S

分子量

491.49

别名

PF 573228

储存和溶解度

DMSO:49.2 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years