[CAS NO. 869288-64-2] PF-573228

Name: PF-573228
Brand: Arctom Scientific
SKU: SLK-S2013

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [869288-64-2]

Store

Catalog

SLK-S2013

Brand

Selleck

CAS

869288-64-2

DESCRIPTION [869288-64-2]

Overview

MDL	MFCD11519967
Molecular Weight	491.49
Molecular Formula	C22H20F3N5O3S
SMILES	N(C=1C=C2C(=CC1)NC(=O)CC2)C=3N=C(NCC4=CC(S(C)(=O)=O)=CC=C4)C(C(F)(F)F)=CN3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.0346 mL	10.1731 mL	20.3463 mL
5 mM	0.4069 mL	2.0346 mL	4.0693 mL
10 mM	0.2035 mL	1.0173 mL	2.0346 mL
50 mM	0.0407 mL	0.2035 mL	0.4069 mL

Description

PF-573228 is an ATP-competitive inhibitor of with of 4 nM in a cell-free assay, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. PF-573228 induces .

Targets

FAK ^[1]
(Cell-free assay)

4 nM

In vitro

PF 573228 blocks the phosphorylation of FAK Tyr in REF52 cells, PC3 cells, SKOV-3 cells, L3.6p1 and F-G, MDCK cells with IC50 of 30-500 nM. However, PF 573228 (1 μM) with 80% inhibition of FAK phosphorylation fails to inhibit cell growth or apoptosis. Similar treatment of cells with PF-228 resulted in inhibition of serum or FN-directed migration and decreased focal adhesion turnover.

In vivo

Inhibition of FAK by PF-573,228 in Ctrl-MT mice leads to a significant suppression of mammary tumorigenesis as well as lung metastasis. In contrast, treatment of MFCKO-MT mice with PF-573,228 did not affect the initiation of mammary tumors in these mice, as would be expected due to the absence of FAK in mammary epithelial cells of these mice .

References

[1] Slack-Davis JK, et al. J Biol Chem, 2007, 282(20), 14845-14852.
[2] Fan H, et al. J Biol Chem. 2011, 286(21):18573-82.

Synonyms

2(1H)-Quinolinone, 3,4-dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-

3,4-Dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-2(1H)-quinolinone

6-[(4-((3-(Methanesulfonyl)benzyl)amino)-5-trifluoromethylpyrimidin-2-yl)amino]-3,4-dihydro-1H-quinolin-2-one

PF 573228