MK-8745 - CAS 885325-71-3
Catalog number: 885325-71-3
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
Inquire
Targets:
Aurora Kinase
Description:
MK-8745 is a novel Aurora-A specific inhibitor. MK8745 induced apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lineages. Exposure of p53 wild-type cells to MK8745 resulted in the induction of p53 phosphorylation (ser15) and an increase in p53 protein expression. p53-dependent apoptosis by MK8745 was further confirmed in HCT 116 p53(-/-) cells transfected with wild-type p53.
Publictions citing BOC Sciences Products
  • >> More
Purity:
0.98
Appearance:
Solid powder
Synonyms:
MK-8745; MK 8745; MK8745.
MSDS:
Inquire
Current Developer:
Merck.
1.A novel Aurora kinase A inhibitor MK-8745 predicts TPX2 as a therapeutic biomarker in non-Hodgkin lymphoma cell lines.
Chowdhury A1, Chowdhury S, Tsai MY. Leuk Lymphoma. 2012 Mar;53(3):462-71. doi: 10.3109/10428194.2011.619018. Epub 2011 Oct 24.
Selective small-molecule kinase inhibitors have encouraging clinical efficacy in several malignancies. These agents are still limited to a subset of patients, indicating the need to develop therapeutic biomarkers that influence clinical benefit. In this study, we demonstrate that treatment with MK-8745, a novel Aurora-A specific inhibitor, leads to cell cycle arrest at the G2/M phase with accumulation of tetraploid nuclei followed by cell death in non-Hodgkin lymphoma (NHL) cell lines. The sensitivity of the cell lines to MK-8745 is correlated with the expression level of Aurora-A activator. The siRNA knockdown of Aurora-A activator TPX2 (targeting protein for Xenopus kinase-like protein 2) increased MK-8745 sensitivity in less-MK-8745-sensitive NHL cell lines, whereas overexpression of TPX2 in high-MK-8745-sensitive NHL cell lines increased drug resistance. Our results indicate that TPX2 may serve as a biomarker for identifying subpopulations of patients sensitive to Aurora-A inhibitor treatment.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Aurora Kinase Products


CAS 656820-32-5 Reversine

Reversine
(CAS: 656820-32-5)

CAS 885325-71-3 MK-8745

MK-8745
(CAS: 885325-71-3)

MK-8745 is a novel Aurora-A specific inhibitor. MK8745 induced apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lin...

CAS 898280-07-4 XL228

XL228
(CAS: 898280-07-4)

XL228 is a protein kinase inhibitor targeting IGF1R, the Aurora kinases, FGFR1-3, ABL and SRC family kinases.

CAS 722543-31-9 Barasertib

Barasertib
(CAS: 722543-31-9)

Barasertib is an orally bioavailable, small-molecule, dihydrogen phosphate prodrug of the pyrazoloquinazoline Aurora kinase inhibitor AZD1152–hydroxyquinazolin...

CAS 869363-13-3 MLN8054

MLN8054
(CAS: 869363-13-3)

MLN8054 is an aurora kinase inhibitor MLN8054, which is an orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase...

CAS 693228-63-6 CYC116

CYC116
(CAS: 693228-63-6)

CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active ...

CAS 398493-79-3 PHA-680632

PHA-680632
(CAS: 398493-79-3)

PHA-680632 is a is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM. PHA-680632 is also the first representative of a ...

CAS 722544-51-6 AZD-1152HQPA

AZD-1152HQPA
(CAS: 722544-51-6)

AZD-1152HQPA is an active metabolite of Barasertib (AZD-1152), which is a novel acetanilide-substituted pyrazole-aminoquinazoline prodrug that is converted rap...

CAS 942918-07-2 GSK-1070916A

GSK-1070916A
(CAS: 942918-07-2)

GSK-1070916A is an ATP-competitive inhibitor of the serine/threonine kinases Aurora B and C with potential antineoplastic activity. Aurora B/C kinase inhibitor ...

CAS 827318-97-8 Danusertib

Danusertib
(CAS: 827318-97-8)

Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Aurora kinase inhibitor PHA-739358 binds to and inhibits the A...

CAS 331771-20-1 ZM447439

ZM447439
(CAS: 331771-20-1)

ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM, 130 nM respectively, > 8 fold selectivity than Aurora C

CAS 1094067-13-6 SCH1473759 (HCl salt)

SCH1473759 (HCl salt)
(CAS: 1094067-13-6)

The hydrochloride salt form of SCH-1473759, a new sub-nanomolar Aurora A/B inhibitor which could result in cell death by inhibiting Aurora kinases. It is proved...

CAS 1291074-87-7 ENMD-2076 L-(+)-Tartaric acid

ENMD-2076 L-(+)-Tartaric acid
(CAS: 1291074-87-7)

ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more selec...

CAS 942947-93-5 CCT129202

CCT129202
(CAS: 942947-93-5)

CCT129202 is an inhibitor of Aurora kinase activity and displays a favorable antineoplastic effect in preclinical studies. CCT129202 significantly reversed ABCB...

CAS 1146618-41-8 SNS-314 Mesylate

SNS-314 Mesylate
(CAS: 1146618-41-8)

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 T...

CAS 1028486-01-2 Alisertib

Alisertib
(CAS: 1028486-01-2)

MLN8237 is a second-generation, orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase with pote...

CAS 1010085-13-8 MK-5198

MK-5198
(CAS: 1010085-13-8)

MK-5108 is a novel small molecule with potent inhibitory activity against Aurora-A kinase. Although most of the Aurora-kinase inhibitors target both Aurora-A an...

SAR156497
(CAS: 1256137-14-0)

SAR156497 is a selective Aurora A, B and C inhibitor with in vitro and in vivo efficacy IC50 value is 0.5 nM for Aurora A; 1.0 nM for Aurora B (incenp) and 3.0 ...

CAS 1094069-99-4 SCH-1473759

SCH-1473759
(CAS: 1094069-99-4)

SCH-1473759 is a novel sub-nanomolar Aurora A/B inhibitor. SCH 1473759 was active against a large panel of tumor cell lines from different tissue origin and gen...

CAS 942487-16-3 PF-03814735

PF-03814735
(CAS: 942487-16-3)

PF-03814735 is an orally bioavailable, ATP-competitive, reversible small-molecule Aurora kinase inhibitor with potential antineoplastic activity. Aurora kinase ...

Chemical Structure

CAS 885325-71-3 MK-8745

Quick Inquiry

Verification code

Featured Items