[CAS NO. 717907-75-0] PF-562271

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 [717907-75-0]

Catalog

HY-10459

Brand

MCE

CAS

717907-75-0

DESCRIPTION [717907-75-0]

Overview

MDL	-
Molecular Weight	507.49
Molecular Formula	C21H20F3N7O3S
SMILES	CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(C=C3)NC(C4)=O)=NC=C2C(F)(F)F)=O

For research use only. We do not sell to patients.

12 Publications Citing Use of MCE

Summary

PF-562271 (VS-6062) is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC ₅₀ s of 1.5 nM and 13 nM, respectively ^[1] .

IC50 & Target

IC50: 1.5 nM (FAK), 13 nM (Pyk2), 30 nM (CDK2), 47 nM (CDK3), 58 nM (CDK1), 97 nM (CDK7), 97 nM (Flt3) ^[1]

In Vitro

PF-562271 (VS-6062) is shown to be a 30- to 120-nM inhibitor of CDK2/E, CDK5/p35, CDK1/B, and CDK3/E in recombinant enzyme assays, in cell-based assays evaluating the role of CDKs, a 48-hour exposure of 3.3 μM PF-562271 is required to alter cell cycle progression. PF-562271 is potent in an inducible cell-based assay measuring phospho-FAK with a IC ₅₀ of 5 nM ^[1] .
PF-562271, a selective inhibitor of both FAK and proline-rich tyrosine kinase 2 (PYK2), a FAK-related family member, on cell growth and colony formation in Ewing sarcoma cell lines. Seven cell lines are treated for 5 days with PF-562271 across a range of concentrations using 2-fold serial dilutions. Treatment with PF-562271 impaires cell viability in all cell lines, with an average IC ₅₀ of 2.4 μM after 3 days of treatment. TC32 and A673 are the 2 most sensitive cell lines, with IC ₅₀ concentrations of 2.1 and 1.7 μM, respectively ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PF-562271 inhibits FAK phosphorylation in vivo in a dose-dependent fashion (calculated EC ₅₀ of 93 ng/mL, total) after p.o. administration to tumor-bearing mice ^[1] . Rats that receive PF-562271 demonstrate a decrease in tumor growth after 2 weeks of treatment with signs of bone healing as evidenced by the deposition of new bone (cortical and cancellous) at sites previously damaged by the tumor ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL ( 246.31 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9705 mL	9.8524 mL	19.7048 mL
5 mM	0.3941 mL	1.9705 mL	3.9410 mL
10 mM	0.1970 mL	0.9852 mL	1.9705 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 1.67 mg/mL (3.29 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 1.67 mg/mL (3.29 mM); Clear solution

* All of the co-solvents are available by MCE.