Aurora B Inhibitor

Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC₅₀=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.

Barasertib (AZD1152), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC₅₀ of 0.37 nM in a cell-free assay. Barasertib (AZD1152) induces growth arrest and apoptosis in cancer cells.

Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC₅₀ of 0.37 nM in a cell-free assay. Barasertib-HQPA (AZD2811) induces growth arrest and apoptosis in cancer cells.

Reversine is a novel class of ATP-competitive Aurora kinase inhibitor with IC₅₀s of 400, 500 and 400 nM for Aurora A, Aurora B and Aurora C, respectively.

Tozasertib (VX 680; MK-0457) is an inhibitor of Aurora A/B/C kinases with K_is of 0.6, 18, 4.6 nM, respectively.

TAS-119 is a potent, selective and orally active Aurora A inhibitor with an IC₅₀ of 1.0 nM. TAS-119 shows high selectivity for Aurora A over other protein kinases, including Aurora B (IC₅₀ of 95 nM). TAS-119 has potent antitumor activites.

Aurora kinase-IN-10 is an Aurora kinase inhibitor. Aurora kinase-IN-10 exhibits IC₅₀ values of 5.94 nM and 86.06 nM against Aurora A and Aurora B, respectively. Aurora kinase-IN-10 has anti-tumor activity and can be used in the research of tumors such as triple-negative breast cancer.

JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2, with IC₅₀s of 9 nM, 3 nM, 11 nM, and 15 nM for CDK1, CDK2, aurora-A and aurora-B, respectively.

ZM-447439 is an aurora kinase inhibitor with IC₅₀s of 110 and 130 nM for aurora A and B, respectively.

Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC₅₀ of 250 nM. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral.

Danusertib is a pyrrolo-pyrazole and aurora kinase inhibitor with IC₅₀ of 13, 79, and 61 nM for Aurora A, B, and C, respectively.

AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor with IC₅₀ of 5 nM, 4 nM and 1 nM for Aurora A, B and C, respectively.

AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC₅₀s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo.

LY3295668 (AK-01) is a highly specific and orally active inhibitor of Aurora-A kinase with a K_i values for AurA and AurB of 0.8 nM and 1038 nM respectively. LY3295668 can effectively inhibit the autophosphorylation of AurA, induce mitotic arrest and apoptosis. LY3295668 avoids the formation of polyploids related to AurB inhibition. LY3295668 can be used for the study of small cell lung cancer.

GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with K_is of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.

TAK-632 is a potent pan-RAF inhibitor with IC₅₀ of 1.4, 2.4 and 8.3 nM for CRAF, BRAF^V600E, BRAF^WT, respectively.

PF-03814735 is a potent, orally available, ATP-competitive and reversible aurora A and aurora B inhibitor with IC₅₀s of 0.8 and 0.5 nM, respectively.

SNS-314 mesylate is a potent and selective aurora kinase inhibitor with IC₅₀s of 9, 31, and 6 nM for aurora A, B and C, respectively.

Tinengotinib (TT00420) is an orally active, spectrally selective small molecule kinase inhibitor targeting Aurora A/B (IC₅₀=1.2-3.3 nM), FGFR1/2/3 (IC₅₀=1.5-3.5 nM), VEGFRs, JAK1/2 and CSF1R. Tinengotinib blocks Aurora kinase-mediated cell cycle progression (inducing G2/M arrest), inhibits FGFR/JNK-JUN signaling pathway and activates MEK/ERK-dependent apoptotic pathway. Tinengotinib has the activity of anti-tumor proliferation, inducing apoptosis, inhibiting angiogenesis and regulating tumor microenvironment. Tinengotinib can be used in the study of triple-negative breast cancer (TNBC), gallbladder cancer and tumor immune microenvironment.

TAK-901 is a multi-targeted aurora inhibitor with IC₅₀s of 21 and 15 nM for aurora A and B, respectively.