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Aurora Kinase

Inhibitory Selectivity
Catalog No.Inhibitor Name Aurora AAurora BAurora COther
A10004Alisertib
****
*
A10981Tozasertib
****
**
***
Bcr-Abl,FLT3
A10109Barasertib
*
****
A11009ZM 447439
**
*
LCK,Src,MEK1
A10601MLN8054
****
*
LCK,PKA,CK2
A10715Danusertib
***
**
**
Abl,TrkA,RET
A10095AT9283
****
****
JAK3,JAK2,Abl1 (T315I)
A10494JNJ-7706621
***
***
CDK2/CyclinE,CDK2/CyclinA,CDK1/CyclinB
A10448Hesperadin
*
TbAUK1
A10100Aurora A Inhibitor I
****
*
*
A10508KW-2449
**
FLT3 (D835Y),Abl (T315I),FLT3
A10851SNS-314 Mesylate
***
**
****
A10352ENMD-2076
***
*
FLT3,RET,VEGFR3/FLT4
A10714PHA-680632
**
*
*
FGFR1,PLK1,FLT3
A11410MK-5108
****
A10248CYC116
***
***
VEGFR2,FLT3,CDK2/CyclinE
A11066AMG-900
***
****
****
p38α,TYK2,JNK2
A11171PF-03814735
****
***
FLT1,FAK,TrkA
A10184CCT129202
**
*
*
A11168GSK1070916
*
****
***
FLT1,Tie-2,SIK
A11067TAK-901
**
***
JAK3,c-Src,YES1
A11081CCT137690
***
**
**
A13396MK-8745
****
*
A10352ENMD-2076 L-(*)-Tartaric acid
***
*
FLT3,RET,VEGFR3/FLT4
A15762BI-847325
**
****
***
A13250Reversine
***
***
**
human A3 adenosine receptor

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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Catalog No. Product Name Application Product Information
A10004 SALE

MLN8237 (Alisertib)

Aurora A Kinase 抑制剂
MLN8237 (Alisertib) 是一种选择性Aurora A抑制剂,无细胞试验中IC50为1.2 nM,作用于Aurora A比作用于Aurora B选择性强200倍以上。Phase 3。
A11168 SALE

GSK1070916

Aurora Kinase B/C 抑制剂

GSK1070916 is a potent Aurora B/C kinase inhibitor (with IC50 of 3.5 nM/6.5 nM) with broad antitumor activity in tissue culture cells and human tumor xenograft models.

A11171

PF-03814735

Aurora A/B Kinase 抑制剂
PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.
A10714 SALE

PHA-680632

Aurora 抑制剂
PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2/3.
A11410 SALE

MK-5108 (VX-689)

Aurora A Kinase 抑制剂
MK-5108, also known as VX-689, is a competitive inhibitor of the ATP-binding site of aurora A kinase.
A10851

SNS-314

Aurora 抑制剂
SNS-314 Mesylate 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.
A11009 SALE

ZM-447439

Aurora Kinase 抑制剂
ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc.
A10248 SALE

CYC116

Aurora Kinase 抑制剂
Aurora kinase/VEGFR 2 inhibitor CYC116 inhibits Aurora kinases A and B and vascular endothelial growth factor receptor 2 (VEGFR2), resulting in disruption of the cell cycle, rapid cell death, and the inhibition of angiogenesis.
A13250 SALE

Reversine

human A3 adenosine receptor 拮抗剂 /Aurora 抑制剂
Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.
A13396 SALE

MK-8745

Aurora Kinase A 抑制剂
MK-8745 is a novel Aurora-A specific inhibitor. It induces apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lineages.
A14382

SAR156497

Aurora Kinase 抑制剂
SAR156497 is an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy with IC50 = 0.5 nM (Aurora A), 1 nM (Aurora B / incenp), 3 nM (Aurora C / incenp) respectively SAR156497 combines high in vitro potency with satisfactory metabolic stability and limited CYP3A4 and PDE3 inhibition.
A15011

AZD1152

Aurora B 抑制剂
AZD1152 is a pro-drug that rapidly undergoes phosphatase-mediated cleavage in serum to release barasertib-hQPA, a selective Aurora B kinase inhibitor that has shown preliminary activity in clinical studies of patients with acute myeloid leukemia (AML).
A15762

BI-847325

MEK/Aurora 抑制剂
BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.
A10184

CCT129202

Aurora 抑制剂

CCT129202 is a representative of a structurally novel series of imidazopyridine small-molecule inhibitors of Aurora kinase activity. It shows high selectivity for the Aurora kinases over a panel of other kinases tested and inhibits proliferation in multiple cultured human tumor cell lines.

A10100

Aurora A Inhibitor I

Aurora A 抑制剂

Aurora A Inhibitor I is a potent and selective inhibitor of Aurora A kinase (AurA), with IC50 values to be 3.4 nM (Aurora A) and unusually high selectivity 1000 fold against Aurora B; a useful tool compound for investigating the cellular role of Aurora A kinases.

A10448 SALE

Hesperadin

Aurora B Kinase 抑制剂
Hesperadin is a human Aurora B inhibitor with an IC50 of 40 nM for the prevention of the phosphorylation of substrate. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo.
A10095 SALE

AT9283

Aurora/JAK 抑制剂
AT9283 inhibits aurora kinase A and B and targets other tyrosine and serine/threonine kinases associated with myeloid cell proliferation.
A10109 SALE

AZD1152-HQPA (Barasertib)

Aurora Kinase B 抑制剂
AZD 1152-HQPA is a highly potent and selective inhibitor of Aurora B, with Ki values to be 0.36 (Aurora B) and 1369 nM (Aurora A) respectively and has a high specificity versus a panel of 50 other kinases.
A10981 SALE

VX-680 (MK-0457, Tozasertib)

Aurora Kinase 抑制剂
VX-680 is a potent and selective small-molecule inhibitor of the Aurora kinases.
A10715 SALE

Danusertib (PHA-739358)

Aurora 抑制剂
Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2
A10601 SALE

MLN8054

Aurora A 抑制剂
MLN8054 is an inhibitor of Aurora A kinase, induces senescence in human tumor cells both in vitro and in vivo.
A10494

JNJ-7706621

CDK/Aurora A/B 抑制剂
JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.
A11081

CCT137690

Aurora Kinase 抑制剂
CCT137690 is a highly selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 15 nM, 25 nM and 19 nM. It has little effect on hERG ion-channel.
A11067 SALE

TAK-901

Aurora Kinase A/B 抑制剂
TAK-901 is a novel inhibitor of Aurora A/B with IC50 of 21 nM/15 nM. It is not a potent inhibitor of cellular JAK2, c-Src or Abl. Phase 1.
A11066

AMG 900

Aurora Kinase 抑制剂
AMG 900 is a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines.
A10508 SALE

KW-2449

FLT3/FGFR/Bcr-Abl/Aurora 抑制剂
KW-2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase.
A10352 SALE

ENMD-2076

Aurora A / FLT3 抑制剂
ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.
A13069 SALE

XL-228

IGF-1R, Aurora, FGFR, ABL, SRC 抑制剂
XL228 is a protein kinase inhibitor targeting IGF1R, the AURORA kinases, FGFR1-3, ABL and SRC family kinases. XL228 is an Aurora A inhibitor (IC50, f3 nmol/L) that has shown potent biochemical activity against ABL1 (Ki, 5 nmol/L), as well as the BCR-ABL1 T315I (Ki, 1.4 nmol/L) kinases.
A13567

TC-A-2317 HCl

Aurora kinase A 抑制剂
TC-A-2317 hydrochloride is a potent Aurora kinase A inhibitor (Ki = 1.2 nM compared to 101 nM for inhibition of Aurora kinase B). Selective over 60 other kinases (IC50 values > 1000 nM). Exhibits good cell permeability and antitumor activity.
A14059

SCH-1473759

Aurora A/B 抑制剂
SCH-1473759 is a novel sub-nanomolar Aurora A/B inhibitor with IC50 of 4 nM and 13 nM, respectively.
A15970

HOI-07

Aurora B 抑制剂
HOI-07 is a potently Aurora B kinase inhibitor.

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