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Request The Product List ofAurora Kinase Aurora Kinase

     Aurora kinases are serine/threonine kinases that are essential for cell proliferation. Aurora kinase helps the dividing cell dispense its genetic materials to its daughter cells. More specifically, Aurora kinases play a crucial role in cellular division by controlling chromatid segregation. Defects in this segregation can cause genetic instability, a condition which is highly associated with tumorigenesis.


    Three Aurora kinases have been identified in mammalian cells to date, Aurora A, Aurora B, Aurora C. Besides being implicated as mitotic regulators, these three kinases have generated significant interest in the cancer research field due to their elevated expression profiles in many human cancers. The human Aurora kinases present a similar domain organization, with a N-terminal domain of 39 to 129 residues in length, a protein kinase domain and a short C-terminal domain containing 15 to 20 residues. The N-terminal domain of three proteins share low sequence conservation, which determines selectivity during protein-protein interactions.

Cat. No. Product Name CAS No. Information
GY06993

AKCI

669750-88-3

AKCI is a small-molecule inhibitor that blocks the Aurora C/IκBα interaction (IC50=24.9 uM) and exerts antitumor activity in MDA-MB-231 breast cancer cells; induces G2/M cell-cycle arrest through modulation of the p53/p21/CDC2/cyclin B1 pathways, significantly inhibits MDA-MB-231 cell migration and invasion, as well as decreasing colony formation and tumor growth, decreases PMA-induced activation of NF-κB.

GY10172

LY3295668

1919888-06-4

LY3295668 (LY-3295668, AK-01) is a novel potent, highly selective, orally active Aurora-A kinase inhibitor with Ki of 0.8 nM, H446 AurA auto-P IC50 of 0.6 nM; displays >1000-fold selectivity over Aur-B, 5/386 kinases were potently inhibited by LY3295668 (<10 nM) and none of these kinases overlapped with targets of the other AurAi (MK5108, alisertib), and no inhibition of SYK; LY3295668 is cytotoxic to RB1 mutant cancer cancaer cells (NCI-H446 cell IC50=0.752 uM), causes durable regression of RB1mut tumor xenografts.

GY02145

SCH-1473759

1094069-99-4

A potent, picomolar, dual inhibitor of Aurora A and B with IC50 of 0.02 and 0.03 nM, respectively; shows improved cell potency (phos-HH3 inhibition IC50=25 nM) and intrinsic aqueous solubility (11.4 mM); emonstrated efficacy and target engagement in human tumor xenograft mouse models.

GY02144

SCH-1473759 hydrochloride

1094067-13-6

A potent, picomolar, dual inhibitor of Aurora A and B with IC50 of 0.02 and 0.03 nM, respectively; shows improved cell potency (phos-HH3 inhibition IC50=25 nM) and intrinsic aqueous solubility (11.4 mM); emonstrated efficacy and target engagement in human tumor xenograft mouse models.

GY01964

ENMD-2076 Tartrate

1291074-87-7

A multitargeted kinase inhibitor with IC50s of 3/14/23/40 nM for Flt3/Aurora A/Src/VEGFR2; also inhibits Aurora B, c-Kit, FGFR1 (IC50=100-350 nM); orally bioactive.

GY01938

CCT129202

942947-93-5

CCT129202 is a potent, selective, ATP-competitive pan-Aurora kinase inhibitor with IC50 of 42, 198 and 227 nM for Aurora A, Aurora B and Aurora C, respectively; displays high selectivity for the Aurora kinases over a broad range of 13 other kinases; inhibits proliferation in multiple cultured human tumor cell lines (GI50=0.08-1.7 uM), induces aberrant mitosis that leads to apoptosis; reduces phosphorylation of histone H3, stabilizes p53, and inhibits growth of HCT116 human colon cancer xenografts in athymic mice.

GY03508

AZD1152

722543-31-9

A potent, highly selective Aurora B inhibitor with IC50 of 0.37 nM; displays >1,000-fold selectivity over Aurora B kinase; induces growth arrest and apoptosis in human acute leukemia cells in vitro and in vivo.

GY05081

AS 703569

871357-89-0

Cenisertib (AS 703569;R763) is a novel potent, orally available inhibitor of Aurora kinases, exhibits signifficant anti-proliferative activity against a wide range of tumor cells both in vitro and in vivo (A549 EC50=9 nM); demonstrates marked inhibition of tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.

GY05047

BI 831266

958227-46-8

BI 831266 is a potent, selective inhibitor of Aurora kinase B (AURKB) with IC50 of binding IC50 of 42 nM; inhibits the proliferation of human non-small cell lung cancer (NSCLC), pancreatic cancer, and prostate cancer cell lines (H460 tumor cell proliferation inhibition IC50=11 nM); causes tumor regression and growth inhibition in in murine xenograft tumor models (HCT 116 colon carcinoma, BxPC3 pancreatic adenocarcinoma, and NCI-H460 NSCLC).

GY01738

SNS-314

1146618-41-8

SNS-314 is a potent, selective pan-Aurora kinase inhibitor with IC50 of 9 and 31 nM for Aurora A and Aurora B, repectively; demonstrates broad activity in vitro against multiple human cancer cell lines and exhibits significant in vivo activity against a wide range of tumor xenograft models; shows additive antiproliferative effects with carboplatin, gemcitabine, 5-FU, daunomycin, and SN-38 both in vitro and in vivo.

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