Aurora Kinase

Inhibitory Selectivity

Catalog No.	Inhibitor Name	Aurora A	Aurora B	Aurora C	Other
A10004	Alisertib	****	*
A10981	Tozasertib	****	**	***	Bcr-Abl,FLT3
A10109	Barasertib	*	****
A11009	ZM 447439	**	*		LCK,Src,MEK1
A10601	MLN8054	****	*		LCK,PKA,CK2
A10715	Danusertib	***	**	**	Abl,TrkA,RET
A10095	AT9283	****	****		JAK3,JAK2,Abl1 (T315I)
A10494	JNJ-7706621	***	***		CDK2/CyclinE,CDK2/CyclinA,CDK1/CyclinB
A10448	Hesperadin		*		TbAUK1
A10100	Aurora A Inhibitor I	****	*	*
A10508	KW-2449	**			FLT3 (D835Y),Abl (T315I),FLT3
A10851	SNS-314 Mesylate	***	**	****
A10352	ENMD-2076	***	*		FLT3,RET,VEGFR3/FLT4
A10714	PHA-680632	**	*	*	FGFR1,PLK1,FLT3
A11410	MK-5108	****
A10248	CYC116	***	***		VEGFR2,FLT3,CDK2/CyclinE
A11066	AMG-900	***	****	****	p38α,TYK2,JNK2
A11171	PF-03814735	****	***		FLT1,FAK,TrkA
A10184	CCT129202	**	*	*
A11168	GSK1070916	*	****	***	FLT1,Tie-2,SIK
A11067	TAK-901	**	***		JAK3,c-Src,YES1
A11081	CCT137690	***	**	**
A13396	MK-8745	****	*
A10352	ENMD-2076 L-(*)-Tartaric acid	***	*		FLT3,RET,VEGFR3/FLT4
A15762	BI-847325	**	****	***
A13250	Reversine	***	***	**	human A3 adenosine receptor

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Catalog No.	Product Name	Application	Product Information
A10494	JNJ-7706621	CDK/Aurora A/B 抑制剂	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.
A10352 SALE	ENMD-2076	Aurora A / FLT3 抑制剂	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.
A10508 SALE	KW-2449	FLT3/FGFR/Bcr-Abl/Aurora 抑制剂	KW-2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase.
A14382	SAR156497	Aurora Kinase 抑制剂	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 CYP3A4 and PDE3 inhibition.
A15762	BI-847325	MEK/Aurora 抑制剂	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.
A11009 SALE	ZM-447439	Aurora Kinase 抑制剂	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.
A10851	SNS-314	Aurora 抑制剂	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.
A11410 SALE	MK-5108 (VX-689)	Aurora A Kinase 抑制剂	MK-5108, also known as VX-689, is a competitive inhibitor of the ATP-binding site of aurora A kinase. Product Citations (1) Wei TW,et al. Aurora A and NF-κB Survival Pathway Drive Chemoresistance in Acute Myeloid Leukemia via the TRAF-Interacting Protein TIFA, Cancer Res, 2017, Jan 15;77(2):494-508 28069801
A10714 SALE	PHA-680632	Aurora 抑制剂	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.
A10248 SALE	CYC116 (CYC-116)	Aurora Kinase 抑制剂	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.
A13069 SALE	XL-228	IGF-1R, Aurora, FGFR, ABL, SRC 抑制剂	XL228 is a protein kinase inhibitor targeting IGF1R, the AURORA kinases, FGFR1-3, ABL and SRC family kinases. XL228 is an Aurora A inhibitor (IC50, f3 nmol/L) that has shown potent biochemical activity against ABL1 (Ki, 5 nmol/L), as well as the BCR-ABL1 T315I (Ki, 1.4 nmol/L) kinases.
A13250 SALE	Reversine	human A3 adenosine receptor 拮抗剂 /Aurora 抑制剂	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.
A13396 SALE	MK-8745	Aurora Kinase A 抑制剂	MK-8745 is a novel Aurora-A specific inhibitor. It induces apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lineages.
A13567	TC-A-2317 HCl	Aurora kinase A 抑制剂	TC-A-2317 hydrochloride is a potent Aurora kinase A inhibitor (Ki = 1.2 nM compared to 101 nM for inhibition of Aurora kinase B). Selective over 60 other kinases (IC50 values > 1000 nM). Exhibits good cell permeability and antitumor activity.
A15011	AZD1152	Aurora B 抑制剂	AZD1152 is a pro-drug that rapidly undergoes phosphatase-mediated cleavage in serum to release barasertib-hQPA, a selective Aurora B kinase inhibitor that has shown preliminary activity in clinical studies of patients with acute myeloid leukemia (AML).
A14059	SCH-1473759	Aurora A/B 抑制剂	SCH-1473759 is a novel sub-nanomolar Aurora A/B inhibitor with IC50 of 4 nM and 13 nM, respectively.
A11171	PF-03814735	Aurora A/B Kinase 抑制剂	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.
A11168 SALE	GSK1070916	Aurora Kinase B/C 抑制剂	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.
A10184	CCT129202	Aurora 抑制剂	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.
A10004 SALE	MLN8237 (Alisertib)	Aurora A Kinase 抑制剂	MLN8237 (Alisertib) 是一种选择性Aurora A抑制剂，无细胞试验中IC50为1.2 nM，作用于Aurora A比作用于Aurora B选择性强200倍以上。Phase 3。 Product Citations (4) Kimura M, .et al. Aurora A regulates the architecture of the Golgi apparatus, Exp Cell Res, 2018, Jun 1;367(1):73-80 PMID: 29571950 Jing Wang, .et al. The Aurora-A–Twist1 axis promotes highly aggressive phenotypes in pancreatic carcinoma, J Cell Sci, 2017, Mar 15; 130(6): 1078–1093 PMID: 28167680 Lessing D, .et al. A high-throughput small molecule screen identifies synergism between DNA methylation and Aurora kinase pathways for X reactivation, Proc Natl Acad Sci U S A, 2016, Dec 13;113(50):14366-14371 PMID: 28182563 Jennifer M. Sahni, .et al. Bromodomain and Extraterminal Protein Inhibition Blocks Growth of Triple-negative Breast Cancers through the Suppression of Aurora Kinases, J Biol Chem, 2016, Nov 4; 291(45): 23756–23768 PMID: 27650498
A10448 SALE	Hesperadin	Aurora B Kinase 抑制剂	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. Product Citations (1) Wenbin Ji,et al. OTSSP167 Abrogates Mitotic Checkpoint through Inhibiting Multiple Mitotic Kinases, PLoS One, 2016, 11(4): e0153518 27082996
A10095 SALE	AT9283	Aurora/JAK 抑制剂	AT9283 inhibits aurora kinase A and B and targets other tyrosine and serine/threonine kinases associated with myeloid cell proliferation.
A10109 SALE	AZD1152-HQPA (Barasertib)	Aurora Kinase B 抑制剂	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. Product Citations (2) Sakamoto K,et al. Recurrent 8q24 rearrangement in blastic plasmacytoid dendritic cell neoplasm: association with immunoblastoid cytomorphology, MYC expression, and drug response, Leukemia, 2018, May 23 29795241 Jennifer M. Sahni,et al. Bromodomain and Extraterminal Protein Inhibition Blocks Growth of Triple-negative Breast Cancers through the Suppression of Aurora Kinases, J Biol Chem, 2016, Nov 4; 291(45): 23756-23768 27650498
A10981 SALE	VX-680 (MK-0457, Tozasertib)	Aurora Kinase 抑制剂	VX-680 is a potent and selective small-molecule inhibitor of the Aurora kinases. Product Citations (2) Sakamoto K,et al. Recurrent 8q24 rearrangement in blastic plasmacytoid dendritic cell neoplasm: association with immunoblastoid cytomorphology, MYC expression, and drug response, Leukemia, 2018, May 23 29795241 W. Joost Lesterhuis,et al. Network analysis of immunotherapy-induced regressing tumours identifies novel synergistic drug combinations, Sci Rep, 2015, 5: 12298 26193793
A10715 SALE	Danusertib (PHA-739358)	Aurora 抑制剂	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 Product Citations (1) Samuel Q. Li, etc. Targeting Wild-Type and Mutationally Activated FGFR4 in Rhabdomyosarcoma with the Inhibitor Ponatinib (AP24534). PLoS One. 2013; 8(10): e76551.
A10601 SALE	MLN8054	Aurora A 抑制剂	MLN8054 is an inhibitor of Aurora A kinase, induces senescence in human tumor cells both in vitro and in vivo.
A11066	AMG 900	Aurora Kinase 抑制剂	AMG 900 is a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines.
A11067 SALE	TAK-901	Aurora Kinase A/B 抑制剂	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.
A11081	CCT137690	Aurora Kinase 抑制剂	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.
A10100	Aurora A Inhibitor I	Aurora A 抑制剂	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.
A15970	HOI-07	Aurora B 抑制剂	HOI-07 is a potently Aurora B kinase inhibitor.

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Aurora Kinase

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Aurora Kinase

A10494

A10352 SALE

A10508 SALE

A14382

A15762

A11009 SALE

A10851

A11410 SALE

A10714 SALE

A10248 SALE

A13069 SALE

A13250 SALE

A13396 SALE

A13567

A15011

A14059

A11171

A11168 SALE

A10184

A10004 SALE

A10448 SALE

A10095 SALE

A10109 SALE

A10981 SALE

A10715 SALE

A10601 SALE

A11066

A11067 SALE

A11081

A10100

A15970