PF-573228 - 10mM in DMSO , CAS No.869288-64-2

CAS: 869288-64-2 Cat. No.: P408655 Formula: C₂₂H₂₀F₃N₅O₃S Molecular Weight: 491.49 EC Number: 663-602-8

GRADE & PURITY 10mM in DMSO

Synonyms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

PF-573228 PF-573228 is an ATP-competitive inhibitor of FAK with IC50 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 apoptosis .
In vitro

PF 573228 blocks the phosphorylation of FAK Tyr³⁹⁷ 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 .
Cell Data

cell lines：VK2 cells

Concentrations：~10 μM

Incubation Time：3 days

Powder Purity:≥98%

Specifications

Synonyms

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

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

PF-573228 is an ATP-competitive inhibitor of FAK with IC50 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 apoptosis.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Names and Identifiers

• Isomeric SMILES: CS(=O)(=O)C1=CC=CC(=C1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC4=C(C=C3)NC(=O)CC4
• WGK Germany: 3
• Molecular Weight: 491.49
• Reaxy-Rn: 12411578
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12411578&ln=

Associated Targets(Human)

PTK2 Tclin Focal adhesion kinase 1 (5 Activities)

Discover Target: PTK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

References

1. Jianghong Wu, Ziwen Long, Hong Cai, Shengjia Yu, Xiaowen Liu.  (2019)  Homeobox B7 accelerates the cancer progression of gastric carcinoma cells by promoting epithelial–mesenchymal transition (EMT) and activating Src–FAK pathway.  OncoTargets and Therapy,      [PMID:31190875] [10.2147/OTT.S198115]

Frequently Asked Questions

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 869288-64-2, the molecular formula is C22H20F3N5O3S, and the molecular weight is 491.49 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.