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WZ3146

WZ3146 Structural

What is WZ3146?

The Uses of WZ3146

WZ3146 is an irreversiblely inhibitor against EGFR T790M.

What are the applications of Application

WZ 3146 is a mutant EGFR phosphorylation inhibitor

Definition

ChEBI: N-[3-[[5-chloro-2-[4-(4-methyl-1-piperazinyl)anilino]-4-pyrimidinyl]oxy]phenyl]-2-propenamide is a member of piperazines.

Biological Activity

wz3146 is a novel, irreversible inhibitor that specifically inhibits phosphorylation of egfr(l858r0) and egfr(e746_a750) with ic50 values of 2nm each.wz3146 has been reported to inhibit the phosphorylation of egfr in the non–small-cell lung cancer (nsclc) cell lines [1]. wz3146 shows to suppress the growth of egfr t790m containing cell lines. besides, analysis of recombinant egfr t790m kinase incubated with wz3146 by electrospray mass spectrometry revealed stoichiometric addition of one inhibitor molecule to the protein. analysis of a pepsin digest of the modified protein by tandem ms identified cys 797 as the site of modification thus verifying covalent bond formation between wz3146 and egfr [2].

References

[1] thanyanan reungwetwattana, saravut j. weroha, julian r. molina. oncogenic pathways, molecularly targeted therapies, and highlighted

Properties of WZ3146

Density  1.318
storage temp.  Store at -20°C
solubility  ≥23.25 mg/mL in DMSO with gentle warming
form  solid
pka 12.78±0.70(Predicted)
color  White to off-white

Safety information for WZ3146

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
Precautionary Statement Codes P280:Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352:IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313:IF SKIN irritation occurs: Get medical advice/attention.
P337+P313:IF eye irritation persists: Get medical advice/attention.

Computed Descriptors for WZ3146

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