Aurora Kinase

Cat. No.

A10004

CAS No.

1028486-01-2

Alisertib (MLN8237)

Synonyms: MLN8237

MLN8237 (Alisertib) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Phase 3..

Cat. No.

A10981

CAS No.

639089-54-6

Tozasertib (VX-680, MK-0457)

Synonyms: VX-680; MK-0457

VX-680 is a potent and selective small-molecule inhibitor of the Aurora kinases.

Cat. No.

A15762

CAS No.

1207293-36-4

BI-847325

BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.

Cat. No.

A10109

CAS No.

722544-51-6

Barasertib-HQPA (AZD1152-HQPA, AZD2811)

Synonyms: AZD2811; INH-34; AZD1152-HQPA

AZD 1152-HQPA is a highly potent and selective inhibitor of Aurora B, with Ki values to be 0.36 (Aurora B) and 1369 nM (Aurora A) respectively and has a high specificity versus a panel of 50 other kinases.

Cat. No.

A13250

CAS No.

656820-32-5

Reversine

Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.

Cat. No.

A10095

CAS No.

896466-04-9

AT9283

AT9283 inhibits aurora kinase A and B and targets other tyrosine and serine/threonine kinases associated with myeloid cell proliferation.

Cat. No.

A10448

CAS No.

422513-13-1

Hesperadin

Hesperadin is a human Aurora B inhibitor with an IC50 of 40 nM for the prevention of the phosphorylation of substrate. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo.

Cat. No.

A10494

CAS No.

443797-96-4

JNJ-7706621

JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.

Cat. No.

A10715

CAS No.

827318-97-8

Danusertib (PHA-739358)

Synonyms: PHA-739358

Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2

Cat. No.

A11066

CAS No.

945595-80-2

AMG 900

AMG 900 is a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines.

Cat. No.

A11410

CAS No.

1010085-13-8

MK-5108 (VX-689)

Synonyms: VX689

MK-5108, also known as VX-689, is a competitive inhibitor of the ATP-binding site of aurora A kinase.

Cat. No.

A13111

CAS No.

882531-87-5

R1530

R1530 is a pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta? FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2.

Cat. No.

A10100

CAS No.

1158838-45-9

TC-S 7010 (Aurora A Inhibitor I)

Synonyms: Aurora A Inhibitor I

Aurora A Inhibitor I is a potent and selective inhibitor of Aurora A kinase (AurA), with IC50 values to be 3.4 nM (Aurora A) and unusually high selectivity 1000 fold against Aurora B; a useful tool compound for investigating the cellular role of Aurora A kinases.

Cat. No.

A10184

CAS No.

942947-93-5

CCT129202

CCT129202 is a representative of a structurally novel series of imidazopyridine small-molecule inhibitors of Aurora kinase activity. It shows high selectivity for the Aurora kinases over a panel of other kinases tested and inhibits proliferation in multiple cultured human tumor cell lines.

Cat. No.

A10248

CAS No.

693228-63-6

CYC116

Aurora kinase/VEGFR 2 inhibitor CYC116 inhibits Aurora kinases A and B and vascular endothelial growth factor receptor 2 (VEGFR2), resulting in disruption of the cell cycle, rapid cell death, and the inhibition of angiogenesis.

Cat. No.

A10352

CAS No.

934353-76-1

ENMD-2076

ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.

Cat. No.

A10508

CAS No.

1000669-72-6

KW-2449

KW-2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase.

Cat. No.

A10601

CAS No.

869363-13-3

MLN8054

MLN8054 is an inhibitor of Aurora A kinase, induces senescence in human tumor cells both in vitro and in vivo.

Cat. No.

A10714

CAS No.

398493-79-3

PHA-680632

PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2/3.

Cat. No.

A10851

CAS No.

1146618-41-8

SNS-314 mesylate

Synonyms: SNS314

SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively. It is less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. Phase 1.

Cat. No.

A11009

CAS No.

331771-20-1

ZM-447439

ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc.

Cat. No.

A11067

CAS No.

934541-31-8

TAK-901

TAK-901 is a novel inhibitor of Aurora A/B with IC50 of 21 nM/15 nM. It is not a potent inhibitor of cellular JAK2, c-Src or Abl. Phase 1.

Cat. No.

A11081

CAS No.

1095382-05-0

CCT137690

CCT137690 is a highly selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 15 nM, 25 nM and 19 nM. It has little effect on hERG ion-channel.

Cat. No.

A11168

CAS No.

942918-07-2

GSK1070916

GSK1070916 is a potent Aurora B/C kinase inhibitor (with IC50 of 3.5 nM/6.5 nM) with broad antitumor activity in tissue culture cells and human tumor xenograft models.

Cat. No.

A11171

CAS No.

942487-16-3

PF-03814735

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.