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VX-680 (MK-0457,Tozasertib)Aurora kinase inhibitor

VX-680 (MK-0457,Tozasertib)

Catalog No. A4111
Size Price Stock Qty
10mM (in 1mL DMSO) $65.00 In stock
50mg $60.00 In stock
100mg $100.00 In stock
250mg $200.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

VX-680 (MK-0457,Tozasertib)

Biological Activity

Description VX-680 is an inhibitor of Aurora with Ki values of 0.6 nM, 4.6 nM, 18 nM, 30 nM and 30 nM for Aurora A, C, B, FLT3 and Bcr-Abl, respectively.
Targets Aurora A Aurora B Aurora C FLT3 Bcr-Abl  
IC50 0.6 nM (Ki) 4.6 nM (Ki) 18 nM (Ki) 30 nM (Ki) 30 nM (Ki)  

VX-680 (MK-0457,Tozasertib) Dilution Calculator

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VX-680 (MK-0457,Tozasertib) Molarity Calculator

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Chemical Properties

Cas No. 639089-54-6 SDF Download SDF
Chemical Name N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide
Canonical SMILES CC1=CC(=NN1)NC2=NC(=NC(=C2)N3CCN(CC3)C)SC4=CC=C(C=C4)NC(=O)C5CC5
Formula C23H28N8OS M.Wt 464.59
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

VX-680 (also known as MK-0457 or tozasertib), discovered through a molecular screening campaign, is a potent inhibitor of pan-aurora kinase as well as other kinases including Src, GSK3β, Flt3, JAK2, BCR-Abl (wild type) and BCR-Abl (T315I mutant). It binds to the inactive conformations of non-aurora kinases preventing activation, which leads to the inhibition of a wide array of kinases. Having been extensively investigated in cell lines and/or xenografts in animal models, VX-680 exhibits high degree of anti-tumor activity against a broad spectrum of tumor types, including ovarian, renal cell carcinoma, thyroid, oral squamous cell, CML (wild-type and mutant BCR-Abl), AML, and MM.

Reference

Myke R. Green, Joseph E. Woolery, and Daruka Mahadevan. Update on aurora kinase targeted therapeutics in oncology. Expert Opin Drug Discov. 2011; 6(3): 291-307