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.
- Cat.No. 产品名称 Information
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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)。
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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。
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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.
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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。
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GC67899
Aurora kinase inhibitor-8
Aurora kinase inhibitor-8 是一种高选择性 Aurora 激酶的抑制剂。
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GC48982
CD532
An inhibitor of Aurora A kinase activity and the Aurora A-N-Myc protein-protein interaction
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GC48971
AZD 1152 (hydrochloride)
A prodrug for a potent Aurora B inhibitor
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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。
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GC62433
AKI603
AKI-603 is an inhibitor of Aurora kinase A (AurA), which is developed to overcome resistance mediated by BCR-ABL-T315I mutation.
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GC62189
CD532 hydrochloride
An inhibitor of Aurora A kinase activity and the Aurora A-N-Myc protein-protein interaction
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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.
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GC50050
Hesperadin hydrochloride
A multi-kinase inhibitor
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GC38519
Ilorasertib hydrochloride
A multi-kinase inhibitor
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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。
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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。
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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。
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GC42933
Binucleine 2
An inhibitor of Drosophila Aurora B kinase
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GC40667
Aurora Kinase Inhibitor II
Blocks Aurora A kinase activity
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GC34692
NU6140
A Cdk2 inhibitor
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GC34159
Ilorasertib (ABT-348)
A multi-kinase inhibitor
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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。
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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.
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GC19092
CCT241736
A dual inhibitor of Aurora kinases and FLT3
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GC15711
Aurora Kinase Inhibitor III
A potent inhibitor of Aurora A kinase
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GC13668
Phthalazinone pyrazole
Potent, selective inhibitor of Aurora kinase A
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GC17828
BI-847325
A selective dual MEK/Aurora kinase inhibitor
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GC10442
MK-8745
An Aurora A kinase inhibitor
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GC17455
TAK-632
A selective pan-Raf inhibitor
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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。
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GC17284
Anacardic acid
A histone acetyltransferase inhibitor
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GC13102
XL228
A tyrosine kinase inhibitor
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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。
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GC14651
Reversine
A purine derivative
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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。
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GC18074
PF-03814735
An inhibitor of Aurora A and B kinases
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GC10008
GSK1070916
A potent inhibitor of Aurora B and C kinases
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GC13332
Aurora A Inhibitor I
A potent and selective inhibitor of Aurora A kinase
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GC15106
CYC116
A potent Aurora kinase inhibitor
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GC11085
TAK-901
A non-selective inhibitor of Aurora kinases
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GC14592
KW 2449
A multi-kinase inhibitor
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GC10479
PHA-680632
An Aurora kinase inhibitor
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GC13837
SNS-314 Mesylate
A pan-Aurora kinase inhibitor
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GC17162
MK-5108 (VX-689)
A potent inhibitor of Aurora kinases
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GC13198
AMG-900
A selective pan-Aurora kinase inhibitor
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GC17196
Hesperadin
A multi-kinase inhibitor
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GC10638
AT9283
A broad spectrum kinase inhibitor
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GC15217
Danusertib (PHA-739358)
A pan-Aurora kinase and Abl inhibitor
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GC12612
JNJ-7706621
A dual inhibitor of CDKs and Aurora kinases
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GC12208
MLN8054
An inhibitor of Aurora A kinase
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GC14566
CCT137690
An inhibitor of Aurora kinases and FLT3