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Epigenetics

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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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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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