Successful, we will reply to you quickly.OK
Please select the quantity.OK
Your message is being sent, please wait.Close
Send mail failed, please send again!Close
Products are for research use only. Not for human use. We do not sell to patients.
(ZM447439; ZM 447439)
ZM-447439 Chemical Structure
|Product name: ZM-447439|
|Cat. No.: HY-10128|
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, MEK1, Src.
IC50 Value: 110 nM( for Aurora A); 130 nM (for Aurora B) 
Target: Aurora Kinase
in vitro: 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.
|M.Wt||513.59||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO ≥100mg/mL Water <1.2mg/mL Ethanol ≥45mg/mL
|1 mg||5 mg||10 mg|
|1 mM||1.9471 mL||9.7354 mL||19.4708 mL|
|5 mM||0.3894 mL||1.9471 mL||3.8942 mL|
|10 mM||0.1947 mL||0.9735 mL||1.9471 mL|
. Georgieva I, et al. ZM447439, a novel promising aurora kinase inhibitor, provokes antiproliferative and proapoptotic effects alone and in combination with bio- and chemotherapeutic agents in gastroenteropancreatic neuroendocrine tumor cell lines. Neuroendocrinology. 2010;91(2):121-30.
. Teperek-Tkacz M, et al. Phosphorylation of histone H3 serine 10 in early mouse embryos: active phosphorylation at late S phase and differential effects of ZM447439 on first two embryonic mitoses. Cell Cycle. 2010 Dec 1;9(23):4674-87.
Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM; has >200-fold higher selectivity for Aurora A than Aurora B.
AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A/B/C with IC50 of 5 nM/4 nM /1 nM; >10-fold selective for Aurora kinases than p38(alpha), Tyk2, JNK2, Met and Tie2.
AT9283 is a small molecule a multi-targeted inhibitor with IC50s of 4, 1.2, 1.1 and approximate 3 nM for Bcr-Abl(T3151), JAK2 and JAK3, Aurora A and Aurora B, respectively.
Aurora A inhibitor I is a selective Aurora A inhibitor (Aurora A: IC50=0.0034 (mu)M; Aurora B IC50=3.4 (mu)M), (B/A ratio=1000).
AZD1152 (barasertib), pro-drug of barasertib-hQPA(HY-10126), is a selective Aurora B kinase inhibitor, AZD1152 inhibited the proliferation various types of human leukemia cells with an IC50 ranging from 3 nM to 40 nM.
AZD1152-HQPA is the active metabolite of AZD-1152, AZD1152-HQPA (Barasertib) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM, ~100 fold more selective for Aurora B over Aurora A.
CCT 137690 is a potent inhibitor of Aurora kinases (IC50 values are 0.015, 0.019 and 0.025 (mu)M at Aurora A, Aurora C and Aurora B respectively).
CCT129202 is a Aurora kinase inhibitor with IC50 of 0.042 (plusmn) 0.022, 0.198 (plusmn) 0.05, and 0.227 (plusmn) 0.064 uM for Aurora A, Aurora B, and Aurora C, respectively.
CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM.
Danusertib (PHA-739358) is a pyrrolo-pyrazole and small molecule Aurora kinases inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively.