|VX-680 (MK-0457,Tozasertib)Aurora kinase inhibitor|
Sample solution is provided at 25 µL, 10mM.
Publications citing ApexBio Products
|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)|
|Cas No.||639089-54-6||SDF||Download SDF|
|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
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.
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