ZM 447439

For research use only.

Catalog No.S1103

29 publications

ZM 447439 Chemical Structure

CAS No. 331771-20-1

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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 98 In stock
USD 70 In stock
USD 110 In stock
USD 270 In stock
USD 470 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's ZM 447439 has been cited by 29 publications

Purity & Quality Control

Choose Selective Aurora Kinase Inhibitors

Biological Activity

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 against CDK1/2/4, Plk1, Chk1, etc.
Features An Aurora selective ATP-competitive inhibitor.
Targets
Aurora A [1]
(Cell-free assay)
Aurora B [1]
(Cell-free assay)
LCK [1]
(Cell-free assay)
Src [1]
(Cell-free assay)
MEK1 [1]
(Cell-free assay)
110 nM 130 nM 880 nM 1.03 μM 1.79 μM
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. [1] 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. [2] 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. [3] A recent study shows that ZM-447439 exhibits growth inhibitory and proapoptotic effect on cervical cancer SiHa cells, and enhances the chemosensitivity to cisplatin. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human EoL-1-cell NULpWpNCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1fhUGlvcGmkaYTpc44hd2ZiaIXtZY4hTW:OLUGtZ4VtdCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUi2O|gh|ryP MVLTRW5ITVJ?
MCF7 cell MnvsVJJwdGmoZYLheIlwdiCjc4PhfS=> M3vQcmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgUWNHPyClZXzsJIxqdmVuIFnDOVA:OC5zOUig{txO NEDsfYEyPjN|N{GyNi=>
human P12-ICHIKAWA cell MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NG\mNVNKdmirYnn0bY9vKG:oIHj1cYFvKFBzMj3JR2hKU0GZQTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlI1PDFizszN NFPaXXBUSU6JRWK=
human KARPAS-45 cell MkPZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWPJcohq[mm2aX;uJI9nKGi3bXHuJGtCWlCDUz20OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzhzMkig{txO NF2ycVBUSU6JRWK=
human ES3 cell MoLsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXfheVNoUW6qaXLpeIlwdiCxZjDoeY1idiCHU{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ4OzJizszN NWfGPHV2W0GQR1XS
human ES8 cell NWTOSVZ3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MojuTY5pcWKrdHnvckBw\iCqdX3hckBGWzhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS5PFA3KM7:TR?= M1jYXXNCVkeHUh?=
human TE-11 cell M3XPb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF62UGpKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE42OzdyMzFOwG0> MVXTRW5ITVJ?
human RS4-11 cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGO1VlJKdmirYnn0bY9vKG:oIHj1cYFvKFKVND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTV2NDFOwG0> M4XQT3NCVkeHUh?=
human MOLT-16 cell NH3RcGJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmLITY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE43ODl4MTFOwG0> M4DGbnNCVkeHUh?=
human RKO cell NYjxVoFDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1rQNGlvcGmkaYTpc44hd2ZiaIXtZY4hWkuRIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD63NFY2PiEQvF2= Ml;ZV2FPT0WU
human MV-4-11 cell NILCXWJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWDOUZA5UW6qaXLpeIlwdiCxZjDoeY1idiCPVj20MVEyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC55OU[zJO69VQ>? M3zBZ3NCVkeHUh?=
human SW954 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYPLe|d5UW6qaXLpeIlwdiCxZjDoeY1idiCVV{m1OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvQDN4M{Wg{txO MYTTRW5ITVJ?
human BE-13 cell M2SySGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGHv[oZKdmirYnn0bY9vKG:oIHj1cYFvKEKHLUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE45PDRzODFOwG0> MYXTRW5ITVJ?
human MOLT-4 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnjtTY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlg6QTd6IN88US=> MVjTRW5ITVJ?
human NBsusSR cell NHjq[JVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkPKTY5pcWKrdHnvckBw\iCqdX3hckBPSnO3c2PSJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE46OTN6NzFOwG0> NWXDXVB3W0GQR1XS
human H9 cell M{\KcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mo\STY5pcWKrdHnvckBw\iCqdX3hckBJQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwOUK5O|kh|ryP MmXPV2FPT0WU
human A172 cell NVjZ[HlET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYnJcohq[mm2aX;uJI9nKGi3bXHuJGEyPzJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkm4OFEyKM7:TR?= M2XFbnNCVkeHUh?=
human ES5 cell NUXDbIRtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1;2VmlvcGmkaYTpc44hd2ZiaIXtZY4hTVN3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6wNFI1QCEQvF2= NXvtUIZCW0GQR1XS
human SBC-1 cell MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWj6OmpTUW6qaXLpeIlwdiCxZjDoeY1idiCVQlOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvODN7Mkig{txO NIi5b2NUSU6JRWK=
human NCI-H209 cell NIWxSGNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{PhR2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjF4NkCyJO69VQ>? NGHpTphUSU6JRWK=
human NKM-1 cell M1q3[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3LYd2lvcGmkaYTpc44hd2ZiaIXtZY4hVkuPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlE3Pzl6IN88US=> MXzTRW5ITVJ?
human NCI-H720 cell M1\5PGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3m1emlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi3NlAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjJyNkK3JO69VQ>? M4f3UHNCVkeHUh?=
human KE-37 cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoLqTY5pcWKrdHnvckBw\iCqdX3hckBMTS1|NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNlE{QDhizszN NEjIWZpUSU6JRWK=
human SW48 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHvkXVJKdmirYnn0bY9vKG:oIHj1cYFvKFOZNEigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlI{OTV3IN88US=> MnjqV2FPT0WU
human IST-SL1 cell Mn:wS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFqwOHhKdmirYnn0bY9vKG:oIHj1cYFvKEmVVD3TUFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjNzN{K3JO69VQ>? MU\TRW5ITVJ?
human SK-NEP-1 cell M1LWO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MU\Jcohq[mm2aX;uJI9nKGi3bXHuJHNMNU6HUD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4{PjR7ODFOwG0> NEPNeJBUSU6JRWK=
human NOMO-1 cell NVjq[3BQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mk\uTY5pcWKrdHnvckBw\iCqdX3hckBPV02RLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlM3PzJ3IN88US=> NX\VZ4l2W0GQR1XS
human DOHH-2 cell M4rVRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWjJcohq[mm2aX;uJI9nKGi3bXHuJGRQUEhvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOFAzPzZizszN NHHNWGpUSU6JRWK=
human ABC-1 cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWLJcohq[mm2aX;uJI9nKGi3bXHuJGFDSy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT60NFM2OiEQvF2= NWnnXnMxW0GQR1XS
human Ramos-2G6-4C10 cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHe5W4lKdmirYnn0bY9vKG:oIHj1cYFvKFKjbX;zMVJIPi12Q{GwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU41ODZyNTFOwG0> NVXrVnN[W0GQR1XS
human EM-2 cell NI\6dnJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGrTbIFKdmirYnn0bY9vKG:oIHj1cYFvKEWPLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlQyPzJzIN88US=> MX7TRW5ITVJ?
human NB14 cell M2nRdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVHCVG1MUW6qaXLpeIlwdiCxZjDoeY1idiCQQkG0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42PTZ{MTFOwG0> MWXTRW5ITVJ?
human MOLT-13 cell NGG1ToVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn\hTY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42PjdyNjFOwG0> M3rFZ3NCVkeHUh?=
human ECC10 cell NYfydXpDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYTJcohq[mm2aX;uJI9nKGi3bXHuJGVESzFyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT62N|M2OyEQvF2= NF;KOnRUSU6JRWK=
human LK-2 cell NFXOfVFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUjiUYtHUW6qaXLpeIlwdiCxZjDoeY1idiCOSz2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU43PDV7NDFOwG0> M4OyOXNCVkeHUh?=
human CTB-1 cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX\Jcohq[mm2aX;uJI9nKGi3bXHuJGNVSi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT62O|A5OiEQvF2= NW\JeVRSW0GQR1XS
human NCI-H1581 cell NGjseJlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Ml7sTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG1PFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjZ5NUWg{txO NEPzO3BUSU6JRWK=
human COLO-800 cell NG\yeYRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGTVUFJKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tPFAxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS55MEO4NkDPxE1? NHvtZodUSU6JRWK=
human NB7 cell Mn\IS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWLZWllqUW6qaXLpeIlwdiCxZjDoeY1idiCQQkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlc2Ojl5IN88US=> NED4OVhUSU6JRWK=
human LAMA-84 cell NUfsdI82T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlTXTY5pcWKrdHnvckBw\iCqdX3hckBNSU2DLUi0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44PTV{IN88US=> MXzTRW5ITVJ?
human HCT-116 cells MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVztWJFUUW6qaXLpeIlwdiCxZjDoeY1idiCKQ2StNVE3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS56MEmwPEDPxE1? M1m5T3NCVkeHUh?=
SK-UT-1 cell MlP2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4\CcmlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvVWStNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQDF3MzFOwG0> M{[xZ3NCVkeHUh?=
human H4 cell M3XuUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF25[mdKdmirYnn0bY9vKG:oIHj1cYFvKEh2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT64NVU4QCEQvF2= Ml3oV2FPT0WU
human CAL-51 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVfJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC13MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPFM5PDVizszN NIi3c|VUSU6JRWK=
human LoVo cells NV\sRYZ6WHKxbHnm[ZJifGmxbjDhd5NigQ>? NIjXOHI4OiCq NETmV5FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzvWo8h[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWE1j[XOnZDDXV3Q5KHKnYXflcpQh[XO|YYmsJGlEPTB;MT65JO69VQ>? MnTSNlUzPzB2MEO=
human HN cell M3TScGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXzJcohq[mm2aX;uJI9nKGi3bXHuJGhPKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS57MkWxJO69VQ>? MYjTRW5ITVJ?
human L-363 cell MkW1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml\hTY5pcWKrdHnvckBw\iCqdX3hckBNNTN4MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPVUyOiEQvF2= MX;TRW5ITVJ?
human NCI-H747 cell MlnqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2HwSWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi3OFch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjB|M{WzJO69VQ>? MlX2V2FPT0WU
human A498 cell MkDyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mm\0TY5pcWKrdHnvckBw\iCqdX3hckBCPDl6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj6zOlY6KM7:TR?= NWDRTnNIW0GQR1XS

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p53 / p21 / p-p38 / p38; 

PubMed: 23759594     


U2OS cells were treated for the indicated time with 1 µM ZM447439. Levels of p53, p21, phosphorylated p38 (p-p38) and total p38 were determined by immunoblotting.

pHistone H3 / CEM ; 

PubMed: 22359551     


Detection of phospho Histone H3(Ser10) in CEM and CEM/AKB4 cells treated for 24 hr with increasing concentrations of ZM447439 by western blotting. Shown are representative blots from three independent experiments.

BubR1 / MAD2 / Cyclin B1 ; 

PubMed: 26188358     


ZM induces mitotic slippage in AML cells. NB4 cells were incubated with different doses of ZM (0.5, 1, 2, 5 and 10 μM) or DMSO for 48h; Whole-cell extracts was subjected to immunoblotting by using indicated antibodies.

23759594 22359551 26188358
Immunofluorescence
p21; 

PubMed: 23759594     


U2OS cells were treated with 1 µM ZM447439 for 24 h. Nuclei were stained with Hoechst 33258. p21 was detected by immunostaining. Bar: 50 µm. 

p53; 

PubMed: 23759594     


U2OS cells were treated for the indicated time with 1 µM ZM447439. Levels of p53, p21, phosphorylated p38 (p-p38) and total p38 were determined by immunoblotting.

Aurora B / Survivin ; 

PubMed: 12719470     


Immunofluorescence images of prometaphase DLD-1 cells stained to detect Aurora B (green), Survivin (red), and DNA (blue) after exposure to ZM447439 for 1 h.

23759594 12719470

Protocol

Kinase Assay:[1]
- Collapse

In vitro kinase assays :

Recombinant Aurora A and B are expressed as NH2-terminal His6-tagged fusion proteins using a baculovirus expression system. Aurora A is purified by affinity chromatography using Ni-NTA agarose, and Aurora B is purified by ion exchange chromatography using CM Sepharose Fast Flow. 1 ng purified recombinant enzyme is added to a reaction cocktail containing 25 mM Tris-HCl, pH 7.5, 12.5 mM KCl, 2.5 mM NaF, 0.6 mM DTT, 6.25 mM MnCl2, 10 μM peptide substrate, 10 μM for Aurora A or 5 μM ATP for Aurora B, and 0.2 μCi γ-[33P]ATP (specific activity ≥2,500 Ci/mmol), and is then incubated at RT for 60 minutes. Reactions are stopped by addition of 20% phosphoric acid, and the products are captured on P30 nitrocellulose filters and assayed for incorporation of 33P with a BetaplateTM counter. No enzyme and no compound control values are used to determine the concentration of ZM447439, which gave 50% inhibition of enzyme activity. Further details are available on request from Nicholas Keen.
Cell Research:[2]
- Collapse
  • Cell lines: BON, QGP-1 and MIP-101 cells
  • Concentrations: 0-5 μM
  • Incubation Time: 72 hours
  • Method: Cell number is evaluated by crystal violet staining. In brief, cells in 96-well plates are fixed with 1% glutaraldehyde. Then cells are stained with 0.1% crystal violet. The unbound dye is removed by washing with water. Bound crystal violet is solubilized with 0.2% Triton X-100. Light extinction which increases linearly with the cell number is analyzed at 570 nm using an ELISA reader.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 103 mg/mL (200.54 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 513.59
Formula

C29H31N5O4

CAS No. 331771-20-1
Storage powder
in solvent
Synonyms N/A
Smiles COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=C(C=C3)NC(=O)C4=CC=CC=C4)OCCCN5CCOCC5

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Aurora Kinase Signaling Pathway Map

Aurora Kinase Inhibitors with Unique Features

Related Aurora Kinase Products

Tags: buy ZM 447439 | ZM 447439 supplier | purchase ZM 447439 | ZM 447439 cost | ZM 447439 manufacturer | order ZM 447439 | ZM 447439 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID