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Varlitinib (ARRY334543)ErbB inhibitor

Varlitinib (ARRY334543)

Catalog No. A8365
Size Price Stock 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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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 >23.4mg/mL in DMSO Storage Store at -20°C
General tips N/A
Shipping Condition N/A

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.