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
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
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.
N-Bromosuccinimide Price
- Product number
- SML1990
- Product name
- GW806742X
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $142
- Updated
- 2025/07/31
- Product number
- SML1990
- Product name
- GW806742X
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $545
- Updated
- 2025/07/31
- Product number
- SYN-1215-M050
- Product name
- GW806742X
- Purity
- ≥95%
- Packaging
- 50mg
- Price
- $918
- Updated
- 2021/12/16
- Product number
- SYN1215
- Product name
- GW806742X
- Packaging
- 10mg
- Price
- $340
- Updated
- 2021/12/16
- Product number
- CS-0044745
- Product name
- GW806742X
- Purity
- 98.09%
- Packaging
- 100mg
- Price
- $450
- Updated
- 2021/12/16
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
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