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Varlitinib (ARRY334543)ErbB inhibitor

Varlitinib (ARRY334543)

Catalog No. A8365
Size Price Stock Qty
5mg $120.00 In stock
10mg $190.00 In stock
50mg $470.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Varlitinib(ARRY334543)

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        

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Chemical Properties

Cas No. 845272-21-1 SDF Download SDF
Synonyms ARRY-334543; ARRY 334543
Chemical Name 4-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
Canonical SMILES CC1COC(=N1)NC2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=NC=CS5)Cl
Formula C22H19ClN6O2S M.Wt 466.94
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For 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.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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.