ChemicalBook > CAS DataBase List > GW806742X

GW806742X

Product Name
GW806742X
CAS No.
579515-63-2
Chemical Name
GW806742X
Synonyms
CS-2659;GW806742X;GW806742X ≥95%;GW806742X >=98% (HPLC);GW806742X, 10 mM in DMSO;GW806742X;GW-806742X;GW 806742X;1-[4-[methyl-[2-(3-sulfamoylanilino)pyrimidin-4-yl]amino]phenyl]-3-[4-(trifluoromethoxy)phenyl]urea;3-((4-(Methyl(4-(3-(4-(trifluoromethoxy)phenyl)ureido)phenyl)amino)pyrimidin-2-yl)amino)benzenesulfonamide;3-[[4-[methyl[4-[[[[4-(trifluoromethoxy)phenyl]amino]carbonyl]amino]phenyl]amino]-2-pyrimidinyl]amino]-benzenesulfonamide;Benzenesulfonamide, 3-[[4-[methyl[4-[[[[4-(trifluoromethoxy)phenyl]amino]carbonyl]amino]phenyl]amino]-2-pyrimidinyl]amino]-
CBNumber
CB23067556
Molecular Formula
C25H22F3N7O4S
Formula Weight
573.55
MOL File
579515-63-2.mol
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GW806742X Property

Density 
1.524±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:100.0(Max Conc. mg/mL);174.35(Max Conc. mM)
form 
Solid
pka
10.09±0.60(Predicted)
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1990
Product name
GW806742X
Purity
≥98% (HPLC)
Packaging
5MG
Price
$142
Updated
2025/07/31
Sigma-Aldrich
Product number
SML1990
Product name
GW806742X
Purity
≥98% (HPLC)
Packaging
25MG
Price
$545
Updated
2025/07/31
Adipogen Life Sciences
Product number
SYN-1215-M050
Product name
GW806742X
Purity
≥95%
Packaging
50mg
Price
$918
Updated
2021/12/16
AK Scientific
Product number
SYN1215
Product name
GW806742X
Packaging
10mg
Price
$340
Updated
2021/12/16
ChemScene
Product number
CS-0044745
Product name
GW806742X
Purity
98.09%
Packaging
100mg
Price
$450
Updated
2021/12/16
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GW806742X Chemical Properties,Usage,Production

Uses

GW806742X, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X has activity against VEGFR2 (IC50=2 nM). GW806742X retards MLKL membrane translocation and inhibits necroptosis[1][2].

Biological Activity

GW806742X, an ATP mimetic, is a potent MLKL inhibitor that binds the MLKL pseudokinase domain with a Kd of 9.3μM. It has anti-VEGFR2 activity (IC50=2 nM). It delays MLKL membrane translocation and inhibits necrosis.

in vitro

GW806742X (0.1-10000 nM) inhibits necroptotic death of wild-type mouse dermal fibroblasts (MDFs) stimulated with TSQ (1 ng/mL TNF, 500 nM compound A (Smac mimetic), 10 μM Q-VD -OPh) in a dose-dependent manner. GW806742X shows inhibition of VEGF induced proliferation of HUVECs with an IC50 of 5 nM.

target

MLKL

9.3 μM (Kd)

VEGFR2

2 nM (IC 50 < /sub> )

IC 50

MLKL: 9.3 μM (Kd); VEGFR2: 2 nM (IC50)

References

[1] Hildebrand JM, et al. Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death. Proc Natl Acad Sci U S A. 2014 Oct 21;111(42):15072-7. DOI:10.1073/pnas.1408987111
[2] Sammond DM, et al. Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase. Bioorg Med Chem Lett. 2005;15(15):3519-3523. DOI:10.1016/j.bmcl.2005.05.096

GW806742X Preparation Products And Raw materials

Raw materials

Preparation Products

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579515-63-2, GW806742XRelated Search:


  • GW806742X
  • CS-2659
  • GW806742X;GW-806742X;GW 806742X
  • 1-[4-[methyl-[2-(3-sulfamoylanilino)pyrimidin-4-yl]amino]phenyl]-3-[4-(trifluoromethoxy)phenyl]urea
  • GW806742X ≥95%
  • Benzenesulfonamide, 3-[[4-[methyl[4-[[[[4-(trifluoromethoxy)phenyl]amino]carbonyl]amino]phenyl]amino]-2-pyrimidinyl]amino]-
  • GW806742X >=98% (HPLC)
  • 3-((4-(Methyl(4-(3-(4-(trifluoromethoxy)phenyl)ureido)phenyl)amino)pyrimidin-2-yl)amino)benzenesulfonamide
  • VEGFR,death,GW806742X,translocation,GW-806742X,Vascular endothelial growth factor receptor,membrane,Inhibitor,TSQ,MLKs,inhibit,HUVEC,Mixed Lineage Kinase,necroptotic
  • 3-[[4-[methyl[4-[[[[4-(trifluoromethoxy)phenyl]amino]carbonyl]amino]phenyl]amino]-2-pyrimidinyl]amino]-benzenesulfonamide
  • GW806742X, 10 mM in DMSO
  • 579515-63-2
  • C25H22F3N7O4S