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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.

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

    A histone acetyltransferase inhibitor

  27. GC13102 XL228 A tyrosine kinase inhibitor
  28. GC16614 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 A purine derivative
  30. GC14709 AZD1152 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 An inhibitor of Aurora A and B kinases
  32. GC10008 GSK1070916 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 A non-selective inhibitor of Aurora kinases
  36. GC14592 KW 2449 A multi-kinase inhibitor
  37. GC10479 PHA-680632 An Aurora kinase inhibitor
  38. GC13837 SNS-314 Mesylate A pan-Aurora kinase inhibitor
  39. GC17162 MK-5108 (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) A pan-Aurora kinase and Abl inhibitor
  44. GC12612 JNJ-7706621 A dual inhibitor of CDKs and Aurora kinases
  45. GC12208 MLN8054 An inhibitor of Aurora A kinase
  46. GC14566 CCT137690 An inhibitor of Aurora kinases and FLT3
  47. GC11310 CCT129202 An Aurora kinase inhibitor
  48. GC16519 ENMD-2076 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) A selective Aurora kinase B inhibitor

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