Tozasertib is a potent pan-ARK inhibitor but favors ARK-1 (Ki = 0.6 nM) over ARK-2 (Ki = 18 nM) or ARK-3 (Ki = 4.6 nM). It shows selectivity against a panel of more than 190 different protein kinases. Tozasertib effectively inhibits proliferation of several different cell lines of clear cell renal carcinoma (IC50 < 10μM), inhibiting H3 histone phosphorylation and increasing apoptosis. By depleting ARK activity, tozasertib disrupts bipolar spindle formation during mitosis, arresting cell cycle progression at the G2/M phase.
1. Pollard, J.R., et al. 2009. J. Med. Chem. 52: 2629-2651. PMID: 19320489 2. Li, Y., et al. 2010. Am J Transl Res. 2: 296-308. PMID: 20589168
Soluble in plain water (10-30 µM), DMSO (100 mg/ml), ethanol (<1 mg/ml) at 25 °C, and methanol.
Store at -20° C
~1.41 g/cm3 (Predicted)
n20D 1.71 (Predicted)
Aurora A : IC50 = 0.6 nM; Aurora B: IC50 = 18 nM; Aurora C : IC50 = 4.6 nM; different ATC cells: IC50 = 25- 150 nM; inhibits the growth of cells expressing wild type and mutated BCR-ABL, including T315I: IC50 = 200 nM
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YinYin, Y. et al. (PubMed 25543471) investigated the effect of VX 680 (Tozasertib; MK0457; MK 0457), an aurora inhibitor, on proliferation and apoptosis of K562, KCL22 cell lines and CD34+ cells from chronic myeloid leukemia (CML) patients in vitro. VX-680 treatment significantly induced apoptosis of K562 and KCL22 cells and inhibited the cell proliferation of all three cell lines in a concentration-dependent manner. -SCBT Publication Review
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