aurora b inhibitor 1

Aurora B inhibitor 1 is an Aurora B (Aurora-1) inhibitor (Ki <0.010 µM) with potential anticancer activity for cancer research.

AT9283 (J-504568) is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).

TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1 2 than HER4, less potent to MEK1 5, c-Met, Aurora B, Lck, CSK etc. Phase 1.

Aurora inhibitor 1 is a potent inhibitor of Aurora A and Aurora B kinases with IC50 values of ≤ 4 nM and ≤ 13 nM, respectively.

Ilorasertib hydrochloride (ABT-348 hydrochloride) is an ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A (IC50s: 1 nM, 7 nM, 120 nM). It also suppresses RET tyrosine kinase, PDGFRβ, and Flt1 (IC50s: 7 nM, 3 nM, and 32 nM).

FAK-IN-22 (Compound 26) is an inhibitor of FAK, JAK3, and Aurora B, with IC50 values of 50.94 nM, 9.99 nM, and 0.49 nM, respectively, effectively suppressing tumorigenesis and metastasis in pancreatic ductal adenocarcinoma (PDAC). It inhibits proliferation in PANC-1 cells with an IC50 of 0.15 μM. FAK-IN-22 induces apoptosis and G2 M phase arrest in PANC-1 cells by inhibiting the FAK PI3K Akt signaling pathway.

Chiauranib is a multi-target inhibitor against tumor angiogenesis and exhibits potent anticancer effects. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF1R, with IC50 values ranging from 1-9 nM.

AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50= 0.36 nM).1AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.2,3AZD 1152 inhibits tumor xenograft growthin vivo.4,5 1.Mortlock, A.A., Foote, K.M., Heron, N.M., et al.Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinaseJ. Med. Chem.50(9)2213-2224(2007) 2.Popescu, R., Heiss, E.H., Ferk, F., et al.Ikarugamycin induces DNA damage, intracellular calcium increase, p38 MAP kinase activation and apoptosis in HL-60 human promyelocytic leukemia cellsMutation Research709-71060-66(2011) 3.Moore, A.S., Blagg, J., Linardopoulos, S., et al.Aurora kinase inhibitors: Novel small molecules with promising activity in acute myeloid and Philadelphia-positive leukemiasLeukemia24(4)671-678(2010) 4.Wilkinson, R.W., Odedra, R., Heaton, S.P., et al.AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosisClin. Cancer. Res13(12)3682-3688(2007) 5.Yang, J., Ikezoe, T., Nishioka, C., et al.AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivoBlood110(6)2034-2040(2007)

JH295 hydrate is a potent, irreversible, and selective NIMA-related kinase 2 (Nek2) inhibitor that inhibits cellular Nek2 by Cys22 alkylation (IC50 = 770 nM). JH295 hydrate is not active against the mitotic kinases Cdk1, Aurora B, or Plk1, and does not interfere with bipolar spindle assembly or the spindle assembly checkpoint [1].

GSK-1070916 (GSK-1070916A) is a reversible and ATP-competitive inhibitor of Aurora B C with IC50 of 3.5 nM 6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex. Phase 1.

GSK2646264 (Compound 44) is a highly effective and specific inhibitor of spleen tyrosine kinase (SYK) with a pIC50 of 7.1. It also inhibits multiple kinases, including LCK (pIC50 5.4), LRRK2 (pIC50 5.4), GSK3β (pIC50 5.3), JAK2 (pIC50 5), VEGFR2 (pIC50 4.5), Aurora B (pIC50 <4.6), and Aurora A (pIC50 <4.3). Notably, GSK2646264 demonstrates skin penetrability, reaching both the epidermis and dermis [1].

AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A B C with IC50 values of 5 nM, 4 nM, and 1 nM, respectively. It exhibits over 10-fold selectivity for Aurora kinases compared to p38α, Tyk2, JNK2, Met, and Tie2. [Phase 1].

CYC116 is a potent inhibitor of Aurora A B with Ki of 8.0 nM 9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt PKB, PKC, no effect on GSK-3α β, CK2, Plk1 and SAPK2A. Phase 1.

PF-03814735 is a novel, potent and reversible inhibitor of Aurora A B with IC50of 0.8 nM 5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.

SAR156497 is an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy with IC50 = 0.5 nM (Aurora A); 1 nM (Aurora B incenp); 3 nM (Aurora C incenp) respectively SAR156497 combines high in vitro potency with satisfactory metabolic stability and limited CYP 3A4 and PDE3 inhibition. In vitro, SAR156497 displayed high antiproliferative activity on a large panel of tumor cell lines without correlation with any particular genetic signature or Aurora kinases expression. It induced significant modulation of Aurora A and Aurora B biomarkers (p-Aurora A and pHH3, respectively) and cell polyploidy, as expected from Aurora A B inhibitors.

XMD-12, also known as DUN57447, Aurora inhibitor (compound 1) or Aurora-IN-1, is an Auroro inhibitor, which targets Aurora A B C. (5.6 18.4 24.6 nM).

Ilorasertib (ABT-348) (ABT-348) is an ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora A Aurora B Aurora C (IC50s: 120 nM 7 nM 1 nM). It also suppresses RET tyrosine kinase, PDGFRβ, and Flt1 (IC50s: 7 nM, 3 nM, and 32 nM).