GW806742X
GW806742X Basic information
- Product Name:
- GW806742X
- Synonyms:
-
- 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
- CAS:
- 579515-63-2
- MF:
- C25H22F3N7O4S
- MW:
- 573.55
- Mol File:
- 579515-63-2.mol
GW806742X Chemical Properties
- 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
GW806742X Usage And Synthesis
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
GW806742XSupplier
- Tel
- 027-86697669 13986148687
- sales@tcaschem.com
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- 18149758185
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- Tel
- 021-52996696，15000506266 15000506266
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- +86-400-851-9921
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- 021-65675885 18964387627
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