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Home >> Signaling Pathways >> Cell Cycle/Checkpoint >> Aurora Kinase

Aurora Kinase(极光激酶)

Aurora kinases are a family of serine-threonine kinases of three highly homologous members, including aurora A kinase, aurora B kinase and aurora C kinase, which are responsible for chromosome assembly and segregation during mitosis. Aurora kinases are characterized by two domains: a regulatory domain in the NH2 terminus and a catalytic domain in the COOH terminus, in which an A-Box and a D-Box found correspondingly in each domain are responsible for protein degradation. Aurora A kinase plays an important role in centrosome function and duplication, mitotic entry and bipolar spindle assembly; while Aurora B kinase is the catalytic component of the chromosomal passenger complex regulating the accurate segregation of the chromatids at mitosis, histone modification and cytokinesis. Aurora C kinase is less studied and expressed restrictedly in the testes.

Products for  Aurora Kinase

  1. Cat.No. 产品名称 Information
  2. GC70030 Tinengotinib Tinengotinib 是一种或多种蛋白激酶的调节剂，例如 Aurora 激酶和 VEGFR 激酶。Tinengotinib 具有研究这些激酶异常介导的疾病的潜力，尤其是癌症相关疾病 (摘自专利 WO2018108079A1)。
  3. GC69068 ENMD-2076 Tartrate ENMD-2076 Tartrate 是多靶点激酶抑制剂，抑制 Aurora A，Flt3，KDR/VEGFR2，Flt4/VEGFR3，FGFR1，FGFR2，Src，PDGFRα 的IC50 值分别为1.86，14，58.2，15.9，92.7，70.8，20.2 and 56.4 nM。
  4. GC25940 SNS-314 SNS-314 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.
  5. GC68147 dAURK-4 hydrochloride dAURK-4 hydrochloride 是 Alisertib 的一种衍生物，是一种有效的选择性 AURKA (Aurora A) 降解剂。dAURK-4 hydrochloride 具有抗癌作用。
  6. GC67899 Aurora kinase inhibitor-8 Aurora kinase inhibitor-8 是一种高选择性 Aurora 激酶的抑制剂。
  7. GC62482 TAS-119 TAS-119 是一种有效的，选择性的，具有口服活性的 Aurora A 抑制剂，IC50 为 1.0 nM。TAS-119 对 Aurora A 的选择性高于其他蛋白激酶，包括 Aurora B (IC50 为 95 nM)。TAS-119 具有有效的抗肿瘤活性。
  8. GC62433 AKI603 AKI-603 is an inhibitor of Aurora kinase A (AurA), which is developed to overcome resistance mediated by BCR-ABL-T315I mutation.
  9. GC62189 CD532 hydrochloride An inhibitor of Aurora A kinase activity and the Aurora A-N-Myc protein-protein interaction
  10. GC62145 Chiauranib

    CS2164

     Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy.
  11. GC50050 Hesperadin hydrochloride A multi-kinase inhibitor
  12. GC38519 Ilorasertib hydrochloride

    ABT-348 hydrochloride

     A multi-kinase inhibitor
  13. GC37606 SCH-1473759 hydrochloride SCH-1473759 hydrochloride是多靶点的的极光激酶 (aurora) 抑制剂，对极光激酶A和B的IC50 值分别为4 和13 nM。
  14. GC35651 Cenisertib

    AS-703569; R-763

     Cenisertib (AS-703569) 是一种多激酶抑制剂，可抑制 Aurora-kinase-A/B，ABL1，AKT，STAT5, FLT3 的活性。 Cenisertib 通过抑制肿瘤肥大细胞 (MC) 中几种不同分子靶标的活性抑制其生长。 Cenisertib 抑制异种移植模型中胰腺癌，乳腺癌，结肠癌，卵巢癌和肺癌以及白血病的肿瘤生长。
  15. GC35216 AAPK-25 AAPK-25 是一种有效选择性的 Aurora/PLK 激酶双重抑制剂，具有抗肿瘤活性。AAPK-25 可引起有丝分裂延迟并阻滞前中期细胞，通过生物标志物组蛋白 H3Ser10 磷酸化反应，随后细胞凋亡激增。AAPK-25 靶向 Aurora-A, -B, -C 的 Kd 值为 23 nM-289 nM，靶向 PLK-1, -2, -3 的 Kd 值为 55-456 nM。
  16. GC40667 Aurora Kinase Inhibitor II

    4-(4-Benzamidoanilino)-6,7-dimethoxyquinazoline

     Blocks Aurora A kinase activity
  17. GC34692 NU6140 A Cdk2 inhibitor
  18. GC34159 Ilorasertib (ABT-348)

    ABT-348

     A multi-kinase inhibitor
  19. GC33379 Aurora B inhibitor 1 AuroraBinhibitor1是一种AuroraB(Aurora-1)抑制剂，Ki值<0.010uM。详细信息请参考专利文献WO2007059299A1中的化合物1-3。
  20. GC33057 LY3295668 (AK-01)

    AK-01

     LY3295668 (AK-01) is a potent, orally active and specific inhibitor of Aurora A kinase with Ki of 0.8 nM and 1038 nM for AURKA and AURKB, respectively.
  21. GC19092 CCT241736 A dual inhibitor of Aurora kinases and FLT3
  22. GC17828 BI-847325 A selective dual MEK/Aurora kinase inhibitor
  23. GC10442 MK-8745 An Aurora A kinase inhibitor
  24. GC17455 TAK-632 A selective pan-Raf inhibitor
  25. GC16378 TC-A 2317 hydrochloride TC-A 2317 hydrochloride 是一种具有口服活性的 Aurora A 激酶抑制剂 (Ki=1.2 nM)。 TC-A 2317 hydrochloride 对 Aurora B 激酶 (Ki=101 nM) 和其他 60 种激酶具有出色的选择性、良好的细胞渗透性和良好的 PK 曲线。抗肿瘤活性。
  26. GC17284 Anacardic acid

    漆树酸; Hydroginkgolic acid; Ginkgolic Acid C15

    A histone acetyltransferase inhibitor
  27. GC13102 XL228

    N4-(5-环丙基-1H-吡唑-3-基)-N2-[[3-异丙基-5-异恶唑基]甲基]-6-(4-甲基-1-哌嗪基)-2,4-嘧啶二胺,XL-228;XL 228

     A tyrosine kinase inhibitor
  28. GC16614 SCH-1473759

    SCH1473759;SCH 1473759

     SCH-1473759 是一种极光抑制剂，对极光 A 和 B 的 IC50 分别为 4 和 13 nM。
  29. GC14651 Reversine

    逆转素

     A purine derivative
  30. GC14709 AZD1152

    5-[[7-[3-[乙基[2-(磷酰氧基)乙基]氨基]丙氧基]-4-喹唑啉基]氨基]-N-(3-氟苯基)-1H-吡唑-3-乙酰胺,AZD-1152;AZD 1152

     AZD1152 (AZD1152) 是 AZD1152-hQPA 的前药，是一种高选择性的 Aurora B 抑制剂，在无细胞试验中 IC50 为 0.37 nM。 AZD1152 (AZD1152) 在癌细胞中诱导生长停滞和凋亡。
  31. GC18074 PF-03814735

    N-[2-[(1S,4R)-6-[[4-(环丁基氨基)-5-(三氟甲基)-2-嘧啶基]氨基]-1,2,3,4-四氢萘-1,4-亚氨-9-基]-2-氧代乙基]乙酰胺

     PF-03814735 是一种有效的、具有口服生物利用度的 Aurora1 和 Aurora2 激酶的可逆抑制剂，IC50 值分别为 0.8nM 和 5nM 。
  32. GC10008 GSK1070916

    GSK-1070916A

     A potent inhibitor of Aurora B and C kinases
  33. GC13332 Aurora A Inhibitor I A potent and selective inhibitor of Aurora A kinase
  34. GC15106 CYC116 A potent Aurora kinase inhibitor
  35. GC11085 TAK-901

    5-[3-(乙基磺酰基)苯基]-3,8-二甲基-N-(1-甲基-4-哌啶基)-9H-吡啶并[2,3-B]吲哚-7-甲酰胺

     A non-selective inhibitor of Aurora kinases
  36. GC14592 KW 2449

    [4-[2-(1H-吲唑-3-基)乙烯基]苯基]-1-哌嗪基甲酮

     A multi-kinase inhibitor
  37. GC10479 PHA-680632

    Pha 680632

     An Aurora kinase inhibitor
  38. GC13837 SNS-314 Mesylate

    N-(3-氯苯基)-N'-[5-[2-(噻吩并3,2-D]嘧啶-4-基氨基)乙基]-2-噻唑基]脲甲磺酸盐(1:1)

     A pan-Aurora kinase inhibitor
  39. GC17162 MK-5108 (VX-689)

    VX-689

     A potent inhibitor of Aurora kinases
  40. GC13198 AMG-900 A selective pan-Aurora kinase inhibitor
  41. GC17196 Hesperadin A multi-kinase inhibitor
  42. GC10638 AT9283 A broad spectrum kinase inhibitor
  43. GC15217 Danusertib (PHA-739358)

    达鲁舍替,5-Amido-pyrrolopyrazole 9d

     A pan-Aurora kinase and Abl inhibitor
  44. GC12612 JNJ-7706621

    JNJ7706621, JNJ 7706621

     A dual inhibitor of CDKs and Aurora kinases
  45. GC12208 MLN8054

    4-[[9-氯-7-(2,6-二氟苯基)-5H-嘧啶并[5,4-D][2]苯并氮杂卓-2-基]氨基]苯甲酸

     An inhibitor of Aurora A kinase
  46. GC14566 CCT137690

    甲磺酸阿贝西尼

     An inhibitor of Aurora kinases and FLT3
  47. GC11310 CCT129202

    2-[4-[6-氯-2-(4-二甲基氨基苯基)-3H-咪唑并[4,5-B]吡啶-7-基]哌嗪-1-基]-N-(噻唑-2-基)乙酰胺,CCT-129202, CCT 129202

     An Aurora kinase inhibitor
  48. GC16519 ENMD-2076

    6-(4-甲基-1-哌嗪基)-N-(5-甲基-1H-吡唑-3-基)-2-[(1E)-2-苯乙烯基]-4-嘧啶胺

     A multi-kinase inhibitor
  49. GC12145 ENMD-2076 L-(+)-Tartaric acid ENMD-2076 L-(+)-Tartaric acid 是一种多靶点激酶抑制剂，对 Aurora A、Flt3、KDR/VEGFR2、Flt4/VEGFR3、FGFR1 的 IC50 为 1.86、14、58.2、15.9、92.7、70.8、56.4 nM , FGFR2, Src, PDGFRα, 分别。
  50. GC14409 ZM 447439 Selective inhibitor of Aurora B kinase
  51. GC14955 Barasertib (AZD1152-HQPA)

    5-[[7-[3-[乙基(2-羟基乙基)氨基]丙氧基]-4-喹唑啉]氨基]-N-(3-氟苯基)-1H-吡唑-3-乙酰胺,AZD1152-HQPA,AZD-1152HQPA, AZD1152 HPQA,INH 34

     A selective Aurora kinase B inhibitor

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