N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1)

Description

SNS-314 is a pan-Aurora kinase inhibitor (IC₅₀s = 9, 31, and 3.4 nM for Aurora A, B, and C, respectively). In a panel of 219 kinases, SNS-314 also inhibits TRKB, TRKA, FLT4, FMS, DDR2, AXL, and C-RAF (IC₅₀s = 5-100 nM). SNS-314 inhibits Aurora B phosphorylation of histone H3 in HCT116 human colorectal carcinoma cells in vitro (EC₅₀ = <16 nM) and in a mouse xenograft model at a dose of 50 mg/kg. It also inhibits tumor growth in A2780 ovarian, A375 melanoma, H1299 lung, MDA-MB-231 breast, and PC3 prostate cancer mouse xenograft models when administered biweekly for six weeks at a dose of 170 mg/kg.

Uses

SNS-314 Mesylate is a potent and selective Aurora kinase inhibitor for the treatment of advanced solid tumors.

References

1) Oslob?et al.?(2008)?Discovery of a potent and selective aurora kinase inhibitor; Bioorg. Med. Chem. Lett.?18?4880 2) Arbitrario?et al.?(2010)?SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo; Cancer Chemother. Pharmacol.?65?707 3) VanderPorten?et al.?(2009)?The Aurora kinase inhibitor SNS-314 shows broad therapeutic potential with chemotherapeutics and synergy with microtubule-targeted agents in a colon carcinoma model; Mol. Cancer Ther.?8?930 4) Liu?et al.?(2017)?Targeting high Aurora kinases expression as an innovative therapy for hepatocellular carcinoma; Oncotarget?8?27953