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.

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SCH-1473759 hydrochloride

Catalog No. A21711
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Aurora inhibitor

SCH-1473759 hydrochloride is an aurora inhibitor with IC50s of 4 and 13 nM for aurora A and B, respectively. 了解更多

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CCT241736

Catalog No. A21097
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dual FLT3/Aurora kinase inhibitor

CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor. 了解更多

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AAPK-25

Catalog No. A19085
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Aurora/PLK dual 抑制剂

AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3Ser10 phosphorylation and followed by a surge in apoptosis. 了解更多

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LY3295668

Catalog No. A16869
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Aurora A 抑制剂

LY3295668，也称为AK-01，是有效的Aurora-A激酶抑制剂。了解更多

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HOI-07

Catalog No. A15970
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Aurora B 抑制剂

HOI-07是有效的Aurora B激酶抑制剂。了解更多

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SCH-1473759

Catalog No. A14059
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Aurora A/B 抑制剂

SCH-1473759是一种新型的亚纳摩尔Aurora A/B抑制剂，IC50分别为4 nM和13 nM。了解更多

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TC-A-2317 HCl

Catalog No. A13567
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Aurora kinase A 抑制剂

TC-A-2317 HCl是一种有效的Aurora激酶A抑制剂（Ki = 1.2 nM，而抑制Aurora激酶B则为101 nM）。选择性超过60种其他激酶（IC50值> 1000 nM）。表现出良好的细胞通透性和抗肿瘤活性。了解更多

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XL-228

Catalog No. A13069
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IGF-1R, Aurora, FGFR, ABL, SRC 抑制剂

XL228是靶向IGF1R，AURORA激酶，FGFR1-3，ABL和SRC家族激酶的蛋白激酶抑制剂。XL228是一种Aurora A抑制剂（IC50，f3 nmol/L），对ABL1（Ki，5 nmol/L）以及BCR-ABL1 T315I（Ki，1.4 nmol/L）激酶显示出有效的生化活性。了解更多

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SNS-314

Catalog No. A10851
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Aurora 抑制剂

SNS-314 Mesylate是Aurora A，Aurora B和Aurora C的有效和选择性抑制剂，IC50分别为9 nM，31 nM和3 nM。它对Trk A/B，Flt4，Fms，Axl，c-Raf和DDR2的效力较低。阶段1。了解更多

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ZM-447439

Catalog No. A11009
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Aurora Kinase 抑制剂

ZM 447439是Aurora A和Aurora B的选择性和ATP竞争性抑制剂，IC50分别为110 nM和130 nM。它对Aurora A/B的选择性是MEK1，Src，Lck的8倍以上，对CDK1/2/4，Plk1，Chk1等的影响很小。了解更多

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CYC116 (CYC-116)

Catalog No. A10248
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Aurora Kinase 抑制剂

CYC116 (CYC-116)是一种有效的Aurora A/B抑制剂，Ki为8.0 nM/9.2 nM，对VEGFR2(Ki为44 nM)作用稍弱。了解更多

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Reversine

Catalog No. A13250
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human A3 adenosine receptor 拮抗剂 /Aurora 抑制剂

Reversine是一种有效的人A3腺苷受体拮抗剂，Ki为0.66μM，是一种泛光A/B/C激酶抑制剂，IC50分别为12 nM/13 nM/20 nM。也用于干细胞去分化。了解更多

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- Hazheen K, .et al. BuGZ facilitates loading of spindle assembly checkpoint proteins to kinetochores in early mitosis, J Biol Chem, 2020, August 20
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MK-8745

Catalog No. A13396
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Aurora Kinase A 抑制剂

MK-8745是一种新的极光特异性抑制剂。当在多种谱系的细胞系中进行体外试验时，它以p53依赖的方式诱导凋亡细胞死亡。了解更多

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SAR156497

Catalog No. A14382
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Aurora Kinase 抑制剂

SAR156497是一种选择性选择性的Aurora A，B和C抑制剂，具有体外和体内功效，IC50分别为0.5 nM（Aurora A），1 nM（Aurora B/incenp），3 nM（Aurora C/incenp）SAR156497组合具有很高的体外药效，具有令人满意的代谢稳定性，并且对CYP3A4和PDE3的抑制作用有限。了解更多

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AZD1152

Catalog No. A15011
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Aurora B 抑制剂

AZD1152是一种前药，可在血清中迅速经历磷酸酶介导的裂解作用，释放出Barasertib-hQPA（一种选择性的Aurora B激酶抑制剂），在急性髓细胞性白血病（AML）患者的临床研究中显示出初步活性。了解更多

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BI-847325

Catalog No. A15762
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MEK/Aurora 抑制剂

BI-847325是一种生物利用型选择性MEK/Aurora双重激酶抑制剂，对于非洲爪蟾Aurora B，人Aurora A和Aurora C以及IC50分别为3 nM，25 nM，15 nM，25 nM和4 nM IC50人MEK1和MEK2。了解更多

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- Hilda Samimi, .et al. Alginate-based 3D cell culture technique to evaluate the half-maximal inhibitory concentration: an in vitro model of anticancer drug study for anaplastic thyroid carcinoma, Thyroid Res, 2021, Dec 3;14(1):27 PMID: 34861882
- Hilda Samimi, .et al. Transcript-level regulation of MALAT1-mediated cell cycle and apoptosis genes using dual MEK/Aurora kinase inhibitor "BI-847325" on anaplastic thyroid carcinoma, DARU J Pharm Sci, 2019, 1-7 PMID: 31077090
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MLN8237 (Alisertib)

Catalog No. A10004
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Aurora A Kinase 抑制剂

MLN8237 (Alisertib)是一种选择性Aurora A抑制剂，在无细胞分析中的IC50为1.2 nM。它对Aurora A的选择性比Aurora B高200倍以上。了解更多

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- Bucko PJ, .et al. Subcellular drug targeting illuminates local kinase action, Elife, 2019, Dec 24;8. pii: e52220 PMID: 31872801
- 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
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Hesperadin

Catalog No. A10448
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Aurora B Kinase 抑制剂

Hesperadin是一种人极光B抑制剂，IC50为40 nM，用于防止底物磷酸化。它显著降低AMPK、Lck、MKK1、MAPKAP-K1、CHK1和PHK的活性，而不抑制MKK1在体内的活性。了解更多

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- Wenbin Ji, .et al. OTSSP167 Abrogates Mitotic Checkpoint through Inhibiting Multiple Mitotic Kinases, PLoS One, 2016, 11(4): e0153518 PMID: 27082996
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AT9283

Catalog No. A10095
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Aurora/JAK 抑制剂

AT9283抑制极光激酶A和B，并靶向与骨髓细胞增殖相关的其他酪氨酸和丝氨酸/苏氨酸激酶。了解更多

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- Tomoya Takeda, .et al. AT9283 exhibits antiproliferative effect on tyrosine kinase inhibitor-sensitive and -resistant chronic myeloid leukemia cells by inhibition of Aurora A and Aurora B, Oncol Rep, 2020, August 18
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AZD1152-HQPA (Barasertib)

Catalog No. A10109
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Aurora Kinase B 抑制剂

AZD1152-HQPA (Barasertib)是Aurora B的高效抑制剂，Ki值分别为0.36（Aurora B）和1369 nM（Aurora A），与一组其他50种激酶相比具有很高的特异性。了解更多

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- 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 PMID: 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 PMID: 27650498
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VX-680 (MK-0457, Tozasertib)

Catalog No. A10981
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Aurora Kinase 抑制剂

VX-680 (MK-0457,Tozasertib)是一种有效的选择性Aurora激酶小分子抑制剂。了解更多

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- 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 PMID: 29795241
- W. Joost Lesterhuis, .et al. Network analysis of immunotherapy-induced regressing tumours identifies novel synergistic drug combinations, Sci Rep, 2015, 5: 12298 PMID: 26193793
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Danusertib (PHA-739358)

Catalog No. A10715
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Aurora 抑制剂

Danusertib (PHA-739358)是Aurora A/B/C的Aurora激酶抑制剂，在无细胞分析中的IC50为13 nM/79nM/61 nM，对Abl，TrkA，c-RET和FGFR1以及更低的浓度具有中等效力对Lck，VEGFR2/3，c-Kit，CDK2等有效。了解更多

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- Samuel Q. Li, etc. Targeting Wild-Type and Mutationally Activated FGFR4 in Rhabdomyosarcoma with the Inhibitor Ponatinib (AP24534). PLoS One. 2013; 8(10): e76551.
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MLN8054

Catalog No. A10601
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Aurora A 抑制剂

MLN8054是一种有效的，选择性Aurora A抑制剂，在Sf9昆虫细胞中IC50为4 nM，作用于Aurora A比作用于Aurora B选择性高40倍，可在体内和体外诱导人肿瘤细胞衰老。了解更多

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JNJ-7706621

Catalog No. A10494
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CDK/Aurora A/B 抑制剂

JNJ-7706621是对CDK1/2具有最高效力的pan-CDK抑制剂，IC50为9 nM/4 nM，并且在无细胞分析中对CDK1/2的选择性是CDK3/4/6的6倍以上。它还能有效抑制极光A/B，对Plk1和Wee1没有活性。了解更多

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- Yuta Tanizaki, .et al. Thyroid hormone receptor α controls larval intestinal epithelial cell death by regulating the CDK1 pathway, Commun Biol, 2022, 5: 112 PMID: 35132135
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ENMD-2076

Catalog No. A10352
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Aurora A / FLT3 抑制剂

ENMD-2076具有针对Aurora A和Flt3的选择性活性，IC50为14 nM和1.86 nM，对Aurora A的选择性是Aurora B的25倍，对VEGFR2/KDR和VEGFR3，FGFR1和FGFR2和PDGFRα的作用较小。阶段2。了解更多

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KW-2449

Catalog No. A10508
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FLT3/FGFR/Bcr-Abl/Aurora 抑制剂

KW-2449是FLT3、ABl、ABl-T315I和Aurora激酶的多激酶抑制剂。了解更多

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AMG 900

Catalog No. A11066
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Aurora Kinase 抑制剂

AMG 900是一种新型有效且高度选择性的泛Aurora激酶抑制剂，在紫杉烷抗性肿瘤细胞系中具有活性。了解更多

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- Tomoya Takeda, .et al. AT9283 exhibits antiproliferative effect on tyrosine kinase inhibitor-sensitive and -resistant chronic myeloid leukemia cells by inhibition of Aurora A and Aurora B, Oncol Rep, 2020, August 18
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TAK-901

Catalog No. A11067
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Aurora Kinase A/B 抑制剂

TAK-901是一种新型Aurora A/B抑制剂，IC50为21 nM/15 nM。它不是细胞JAK2，c-Src或Abl的有效抑制剂。了解更多

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CCT137690

Catalog No. A11081
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Aurora Kinase 抑制剂

CCT137690是Aurora A，Aurora B和Aurora C的高度选择性抑制剂，IC50为15 nM，25 nM和19 nM。它对hERG离子通道影响很小。了解更多

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TC-S 7010 (Aurora A Inhibitor I)

Catalog No. A10100
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Aurora A 抑制剂

TC-S 7010 (Aurora A Inhibitor I)是Aurora A激酶（AurA）的有效和选择性抑制剂，IC50值为3.4 nM（Aurora A），对Aurora B具有极高的选择性1000倍；用于研究Aurora A激酶的细胞作用的有用工具化合物。了解更多

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CCT129202

Catalog No. A10184
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Aurora 抑制剂

CCT129202是一种ATP竞争性的pan-Aurora抑制剂，作用于Aurora A，Aurora B和Aurora C时，IC50分别为0.042 μM，0.198 μM和0.227 μM，对FGFR3， GSK3β， PDGFRβ等作用效果稍弱。了解更多

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GSK1070916

Catalog No. A11168
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Aurora Kinase B/C 抑制剂

GSK1070916是一种有效的Aurora B/C激酶抑制剂（IC50为3.5 nM/6.5 nM），在组织培养细胞和人肿瘤异种移植模型中具有广泛的抗肿瘤活性。了解更多

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PF-03814735

Catalog No. A11171
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Aurora A/B Kinase 抑制剂

PF-03814735是一种新颖，有效且可逆的Aurora A/B抑制剂，IC50为0.8 nM/5 nM，对Flt3，FAK，TrkA的效力较低，对Met和FGFR1的活性最低。了解更多

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PHA-680632

Catalog No. A10714
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Aurora 抑制剂

PHA-680632是Aurora A，Aurora B和Aurora C的有效抑制剂，IC50分别为27 nM，135 nM和120 nM。对于FGFR1，FLT3，LCK，PLK1，STLK2和VEGFR2/3，它的IC50高10到200倍。了解更多

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MK-5108 (VX-689)

Catalog No. A11410
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Aurora A Kinase 抑制剂

MK-5108，也称为VX-689，是Aurora A激酶ATP结合位点的竞争性抑制剂。了解更多

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- 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 PMID: 28069801