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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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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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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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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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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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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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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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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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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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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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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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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