[CAS NO. 939791-38-5] PF-562271 besylate

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PRODUCTS SPECIFICATIONS [939791-38-5]

Catalog

HY-10458

Brand

MCE

CAS

939791-38-5

DESCRIPTION [939791-38-5]

Overview

MDL	MFCD14105612
Molecular Weight	665.66
Molecular Formula	C27H26F3N7O6S2
SMILES	CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O.O=S(C5=CC=CC=C5)(O)=O

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

12 Publications Citing Use of MCE

Summary

PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC ₅₀ 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) besylate is a 30- to 120-nM (15.2 to 60.1 ng/mL) inhibitor of cdk2/E, cdk5/p35, cdk1/B, and cdk3/E in recombinant enzyme assays ^[1] . PF-562,271 blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays ^[2] . Treatment of cells with PF-562,271 or knock-down of FAK by siRNA is observed to increase cell-cell adhesion strength ^[3] .

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

In Vivo

PF-562,271 (33 mg/kg, p.o.) inhibits FAK phosphorylation in tumors in a dose- and time-dependent manner in tumor-bearing mice. FAK phosphorylation inhibition relative to total blood concentration of PF-562,271 results in a calculated EC ₅₀ of 93 ng/mL. PF-562,271 (25 mg/kg, p.o.) induces apoptosis 2-fold greater in treated tumors compared with vehicle-treated control tumors on day 3 ^[1] . PF-562,271 (33 mg/kg, p.o.) and dasatinib extensively inhibit the movement of tumor cells in the animals. Inhibition of FAK kinase activity following treatment with PF-562,271 results in altered E-cadherin dynamics in vivo ^[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

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 21.4 mg/mL ( 32.15 mM ; Need ultrasonic and warming)

H ₂ O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5023 mL	7.5113 mL	15.0227 mL
5 mM	0.3005 mL	1.5023 mL	3.0045 mL
10 mM	0.1502 mL	0.7511 mL	1.5023 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 (2.51 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1.67 mg/mL (2.51 mM); Clear solution
3.

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

Solubility: ≥ 1.67 mg/mL (2.51 mM); Clear solution

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

References

Synonyms

Methanesulfonamide, N-[3-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]-2-pyridinyl]-N-methyl-, benzenesulfonate (1:1)

PF 00562271