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Varlitinib (ARRY334543)

In stock
Catalog No.
A8365
ErbB inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$180.00
In stock
5mg
$120.00
In stock
10mg
$190.00
In stock
50mg
$470.00
In stock

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Background

Varlitinib is an orally bioavailable inhibitor of the epidermal growth factor receptor family with potential antineoplastic activity. Varlitinib selectively and reversibly binds to both EGFR (ErbB-1) and Her-2/neu (ErbB-2) and prevents their phosphorylation and activation, which may result in inhibition of the associated signal transduction pathways, inhibition of cellular proliferation and cell death. EGFR and Her-2 play important roles in cell proliferation and differentiation and are upregulated in various human tumor cell types. Due to the dual inhibition of both EGFR and Her-2, this agent may be therapeutically more effective than agents that inhibit EGFR or Her-2 alone.

Chemical Properties

StorageStore at -20°C
M.Wt466.94
Cas No.845272-21-1
FormulaC22H19ClN6O2S
SynonymsARRY-334543; ARRY 334543
Solubility≥23.35mg/mL in DMSO
Chemical Name4-N-[3-chloro-4-(1,3-thiazol-2-ylmethoxy)phenyl]-6-N-[(4R)-4-methyl-4,5-dihydro-1,3-oxazol-2-yl]quinazoline-4,6-diamine
SDFDownload SDF
Canonical SMILESCC1COC(=N1)NC2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=NC=CS5)Cl
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description Varlitinib is a selective and potent inhibitor of ErbB1(EGFR) and ErbB2(HER2) with IC50 values of 7 nM and 2 nM, respectively.
Targets ErbB2 ErbB1        
IC50 2 nM 7 nM        

Quality Control

Quality Control & MSDS

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Chemical structure

Varlitinib(ARRY334543)