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Epigenetics

Epigenetics

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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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