Products

Enzymes for Research, Diagnostic and Industrial Use

ZM-447439

Cat No.
CEI-0891
Description
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 againstCDK1/2/4, Plk1, Chk1, etc.
CAS No.
331771-20-1
Molecular Weight
513.59
Storage
2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO.
Targets
Aurora A, Aurora B
IC50
110 nM; 130 nM
Molecular Formula
C29H31N5O4
Chemical Name
N-(4-(6-methoxy-7-(3-morpholinopropoxy)quinazolin-4-ylamino)phenyl)benzamide
Solubility
DMSO 103 mg/mL; Water <1 mg/mL; Ethanol <1 mg/mL
In vitro
In vitro, ZM-447439 selectively inhibits recombinant human Aurora A and B with IC50 values of 110 and 130 nM, respectively, while other protein kinases of diverse structural types including the mitotic kinases CDK1 and PLK1 are inhibited with IC50 values >10 μM. Aurora kinase inhibitor, ZM-447439 time- and dose-dependently inhibits the growth of all three cell lines with IC50 values of 3 μM (BON), 0.9 μM (QGP-1) and 3 μM (MIP-101) after 72 hours of continuous exposure. In addition, ZM-447439 potently induces cell apoptosis by promoting DNA fragmentation and caspase 3 and 7 activation, and arrests GEP-NET cells in the G0 /G1and G2/M phase of the cell cycle.In mouse embryo, inhibition of Aurora kinase activity by ZM-447439 results in abnormalities during mitosis by regulating the phosphorylation of histone H3 serine 10 (H3S10Ph) from G2 to metaphase with different perturbations in each embryonic cycle.A recent study shows that ZM-447439 exhibits growth inhibitory and proapoptotic effect on cervical cancer SiHa cells, and enhances the chemosensitivity to cisplatin.
Download Datasheet:



Inquiry
Realted Products
Catalog
ProductName
EC No.
CAS No.
Source
Price
CatalogCEI-0335
ProductNamePHA-680632
EC No.
CAS No.398493-79-3
Source
CatalogCEI-0336
ProductNameTAK-901
EC No.
CAS No.934541-31-8
Source
CatalogCEI-0830
ProductNameMK-5108 (VX-689)
EC No.
CAS No.1010085-13-8
Source
CatalogCEI-0832
EC No.
CAS No.1028486-01-2
Source
+ See More >>
Online Inquiry
Name:
*Phone:
*E-mail Address:
Country:
Company/Institution:
*Products or Services Interested:
Quantity:
Project Description:
Our Products are Not Intended for Private Therapeutic Use!
*Verification Code:
Please input "enzymes"(case insensitive) as verification code.

Welcome! For price inquiries, please feel free to contact us through the form below through the form on the left side. We will get back to you as soon as possible.

Sitemap  Privacy Policy
Copyright ©2011 - 2017 Creative Enzymes.
Contact Us 45-1 Ramsey Road, Shirley, NY 11967, USA
Email: info@creative-enzymes.com
Tel: 1-631-562-8517 1-631-448-7888
Fax: 1-631-938-8127
Distributors To view the contact information for a specific location, select the desired country: