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

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PRODUCTS SPECIFICATIONS [869288-64-2]

Catalog

HY-10461

Brand

MCE

CAS

869288-64-2

DESCRIPTION [869288-64-2]

Overview

MDL	MFCD11519967
Molecular Weight	491.49
Molecular Formula	C22H20F3N5O3S
SMILES	O=C1NC2=C(C=C(NC3=NC=C(C(F)(F)F)C(NCC4=CC=CC(S(=O)(C)=O)=C4)=N3)C=C2)CC1

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

13 Publications Citing Use of MCE

Summary

PF-573228 is a potent and selective FAK inhibitor with IC ₅₀ of 4 nM for purified recombinant catalytic fragment of FAK .

IC50 & Target

IC50: 4 nM (FAK) ^[1]

In Vitro

PF-573228 inhibits purified recombinant catalytic fragment of FAK with an IC ₅₀ of 4 nM. In cultured cells, PF-573228 inhibits FAK phosphorylation on Tyr ₃₉₇ with an IC ₅₀ of 30-100 nM. Treatment of cells with concentrations of PF-573228 that significantly decreased FAK Tyr ₃₉₇ phosphorylation fails to inhibit cell growth or induce apoptosis. In contrast, treatment with PF-573228 inhibits both chemotactic and haptotactic migration concomitant with the inhibition of focal adhesion turnover ^[1] .

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 : 25 mg/mL ( 50.87 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent 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

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

In Vivo:

1.

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

Solubility: 2.5 mg/mL (5.09 mM); Suspended solution; Need ultrasonic
2.

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

Solubility: ≥ 2.08 mg/mL (4.23 mM); Clear solution
3.

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

Solubility: ≥ 2.08 mg/mL (4.23 mM); Clear solution

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

References

[1] Slack-Davis JK, et al. Cellular characterization of a novel focal adhesion kinase inhibitor. J Biol Chem. 2007 May 18;282(20):14845-52.

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