Name:Tozasertib
Synonyms:VX-680, MK-0457
CAS Number:639089-54-6
Formula:C23H28N8OS
M.w.:464.59
DMSO (mg/mL)Max Solubility:93
DMSO (mM)Max Solubility:200.18
Form:free base
SMILES:CN1CCN(CC1)C2=NC(=NC(=C2)NC3=N[NH]C(=C3)C)SC4=CC=C(NC(=O)C5CC5)C=C4
ALogP:4.445
Target:Aurora Kinase,Autophagy,Bcr-Abl,FLT3
Pathway:Cell Cycle
Information:Tozasertib (VX-680, MK-0457) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and BCR-ABL tyrosine kinase, which are inhibited by the Tozasertib with both Ki of 30 nM. Tozasertib induces apoptosis and autophagy. Phase 2.
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