MK-8745 - CAS 885325-71-3
Catalog number: 885325-71-3
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C20H19ClFN5OS
Molecular Weight:
431.91416
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.
Purity:
0.98
Appearance:
Solid powder
Synonyms:
MK-8745; MK 8745; MK8745.
MSDS:
Inquire
InChIKey:
YCRFPWKUUNKNDN-UHFFFAOYSA-N
InChI:
InChI=1S/C20H19ClFN5OS/c21-16-5-2-4-15(18(16)22)19(28)27-10-8-26(9-11-27)13-14-3-1-6-17(24-14)25-20-23-7-12-29-20/h1-7,12H,8-11,13H2,(H,23,24,25)
Canonical SMILES:
C1CN(CCN1CC2=NC(=CC=C2)NC3=NC=CS3)C(=O)C4=C(C(=CC=C4)Cl)F
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 896466-04-9 AT9283

AT9283
(CAS: 896466-04-9)

AT-9283 is a broad spectrum kinase inhibitor that potently inhibits Aurora A, Aurora B, JAK2, JAK3, and c-ABL (IC50= 3, 3, 1.2, 1.1, and 4 nM, respectively). It...

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 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 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 1158838-45-9 Aurora A Inhibitor I

Aurora A Inhibitor I
(CAS: 1158838-45-9)

Aurora A Inhibitor I is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM. It is 1000-fold more selective for Aurora A than Aurora B.

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 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 ...

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 ...

Chemical Structure

CAS 885325-71-3 MK-8745

Quick Inquiry

Verification code

Featured Items