ZM 447439

For research use only.

Catalog No.S1103

48 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.

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Selleck's ZM 447439 has been cited by 48 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 M4rxUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYHJcohq[mm2aX;uJI9nKGi3bXHuJGVwVC1zLXPlcIwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF6Nke4JO69VQ>? MVvTRW5ITVJ?
MCF7 cell Mn3oVJJwdGmoZYLheIlwdiCjc4PhfS=> Moq2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDNR2Y4KGOnbHygcIlv\SxiSVO1NF0xNjF7ODFOwG0> NFXiO2UyPjN|N{GyNi=>
human P12-ICHIKAWA cell NXLkdXptT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYTZbXdFUW6qaXLpeIlwdiCxZjDoeY1idiCSMUKtTWNJUUuDV1GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIzPDRzIN88US=> M371ZXNCVkeHUh?=
human KARPAS-45 cell MnnuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NU\uTXh2UW6qaXLpeIlwdiCxZjDoeY1idiCNQWLQRXMuPDViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkO4NVI5KM7:TR?= Ml\qV2FPT0WU
human ES3 cell M3;2R2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mnn2TY5pcWKrdHnvckBw\iCqdX3hckBGWzNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS3N|Ih|ryP M3rZOXNCVkeHUh?=
human ES8 cell NHHsS3hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnzETY5pcWKrdHnvckBw\iCqdX3hckBGWzhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS5PFA3KM7:TR?= M3K4SXNCVkeHUh?=
human TE-11 cell M2LsSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3WwSGlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU{PzB|IN88US=> MUjTRW5ITVJ?
human RS4-11 cell MknHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NISwTlFKdmirYnn0bY9vKG:oIHj1cYFvKFKVND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTV2NDFOwG0> MYnTRW5ITVJ?
human MOLT-16 cell MnnvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MX\Jcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlYxQTZzIN88US=> NX70XnI5W0GQR1XS
human RKO cell MkTBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWDJcohq[mm2aX;uJI9nKGi3bXHuJHJMVyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwN{C2OVYh|ryP MofEV2FPT0WU
human MV-4-11 cell NXzVVI9VT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{e3VWlvcGmkaYTpc44hd2ZiaIXtZY4hVVZvND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzl4MzFOwG0> MlO1V2FPT0WU
human SW954 cell MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX30TYVwUW6qaXLpeIlwdiCxZjDoeY1idiCVV{m1OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvQDN4M{Wg{txO NFT5WGpUSU6JRWK=
human BE-13 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnLiTY5pcWKrdHnvckBw\iCqdX3hckBDTS1zMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuPFQ1OThizszN M{ThTXNCVkeHUh?=
human MOLT-4 cell M4HYRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXjJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuPFk6PzhizszN MkW1V2FPT0WU
human NBsusSR cell Mn73S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4XC[mlvcGmkaYTpc44hd2ZiaIXtZY4hVkK|dYPTVkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvQTF|OEeg{txO M{D0dnNCVkeHUh?=
human H9 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXPiUIdGUW6qaXLpeIlwdiCxZjDoeY1idiCKOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuPVI6PzlizszN NGDwdYdUSU6JRWK=
human A172 cell NWDtO4JwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXPJcohq[mm2aX;uJI9nKGi3bXHuJGEyPzJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkm4OFEyKM7:TR?= MmHQV2FPT0WU
human ES5 cell MoH4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NILvW5RKdmirYnn0bY9vKG:oIHj1cYFvKEWVNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFAzPDhizszN NX7wUJh1W0GQR1XS
human SBC-1 cell Mm\0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHz0dXpKdmirYnn0bY9vKG:oIHj1cYFvKFOEQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4xOzl{ODFOwG0> NF3xbWhUSU6JRWK=
human NCI-H209 cell NETuenFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn\BTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKwPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOTZ4MEKg{txO NHH4eldUSU6JRWK=
human NKM-1 cell NF;DeIxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmezTY5pcWKrdHnvckBw\iCqdX3hckBPU01vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNVY4QThizszN M1L3cXNCVkeHUh?=
human NCI-H720 cell NIHjZWpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{S4ZWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi3NlAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjJyNkK3JO69VQ>? NHWzRnRUSU6JRWK=
human KE-37 cell Mnn4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUezOIduUW6qaXLpeIlwdiCxZjDoeY1idiCNRT2zO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOjF|OEig{txO M4LlPHNCVkeHUh?=
human SW48 cell M3\1e2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml;1TY5pcWKrdHnvckBw\iCqdX3hckBUXzR6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6yN|E2PSEQvF2= M363eHNCVkeHUh?=
human IST-SL1 cell Ml;yS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3ixemlvcGmkaYTpc44hd2ZiaIXtZY4hUVOWLWPMNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOzF5Mkeg{txO MW\TRW5ITVJ?
human SK-NEP-1 cell M4nYUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFrlVJRKdmirYnn0bY9vKG:oIHj1cYFvKFONLV7FVE0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5|NkS5PEDPxE1? MUXTRW5ITVJ?
human NOMO-1 cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHz1WGlKdmirYnn0bY9vKG:oIHj1cYFvKE6RTV:tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOzZ5MkWg{txO NXLIO5ZZW0GQR1XS
human DOHH-2 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV7YRmliUW6qaXLpeIlwdiCxZjDoeY1idiCGT1jIMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjRyMke2JO69VQ>? NIjxWphUSU6JRWK=
human ABC-1 cell MlnQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGrvVXVKdmirYnn0bY9vKG:oIHj1cYFvKEGEQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU41ODN3MjFOwG0> NWe3dlZiW0GQR1XS
human Ramos-2G6-4C10 cell NITX[3JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHzLTGZKdmirYnn0bY9vKG:oIHj1cYFvKFKjbX;zMVJIPi12Q{GwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU41ODZyNTFOwG0> NIHCVotUSU6JRWK=
human EM-2 cell NFi3cYFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX\Jcohq[mm2aX;uJI9nKGi3bXHuJGVONTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkSxO|IyKM7:TR?= MoPrV2FPT0WU
human NB14 cell Ml3VS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVvJcohq[mm2aX;uJI9nKGi3bXHuJG5DOTRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkW1OlIyKM7:TR?= MYTTRW5ITVJ?
human MOLT-13 cell NHnQOJpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{fMWmlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPTZ5ME[g{txO MnnoV2FPT0WU
human ECC10 cell M13kU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFrxR4dKdmirYnn0bY9vKG:oIHj1cYFvKEWFQ{GwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU43OzN3MzFOwG0> NFSzO2pUSU6JRWK=
human LK-2 cell M1riWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1jMTmlvcGmkaYTpc44hd2ZiaIXtZY4hVEtvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOlQ2QTRizszN M2XDcHNCVkeHUh?=
human CTB-1 cell NGT6XVdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVHzOpRwUW6qaXLpeIlwdiCxZjDoeY1idiCFVFKtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPjdyOEKg{txO M3[5fHNCVkeHUh?=
human NCI-H1581 cell MnLWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWLJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUW4NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPjd3NTFOwG0> M2rJbHNCVkeHUh?=
human COLO-800 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1jkcGlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz24NFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjdyM{iyJO69VQ>? NFjMcHpUSU6JRWK=
human NB7 cell MnP5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXvLVXE4UW6qaXLpeIlwdiCxZjDoeY1idiCQQkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlc2Ojl5IN88US=> MXnTRW5ITVJ?
human LAMA-84 cell NI\6cVdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYXJcohq[mm2aX;uJI9nKGi3bXHuJGxCVUFvOESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlc2PTJizszN MVHTRW5ITVJ?
human HCT-116 cells NXrGdXlDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVTJcohq[mm2aX;uJI9nKGi3bXHuJGhEXC1zMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlgxQTB6IN88US=> M1GzWHNCVkeHUh?=
SK-UT-1 cell NEiwVYxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3;RbmlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvVWStNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQDF3MzFOwG0> NIjvSmhUSU6JRWK=
human H4 cell M{fFfGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUT0[3BYUW6qaXLpeIlwdiCxZjDoeY1idiCKNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPFE2PzhizszN M3;G[XNCVkeHUh?=
human CAL-51 cell NVHGOphWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFruXoNKdmirYnn0bY9vKG:oIHj1cYFvKEODTD21NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQDN6NEWg{txO Mo\TV2FPT0WU
human LoVo cells MlTIVJJwdGmoZYLheIlwdiCjc4PhfS=> NF3DWFk4OiCq MlLuRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCOb2\vJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGStZoF{\WRiV2PUPEBz\WGpZX70JIF{e2G7LDDJR|UxRTFwOTFOwG0> MkLvNlUzPzB2MEO=
human HN cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGhPKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS57MkWxJO69VQ>? MYXTRW5ITVJ?
human L-363 cell NGftW5NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHvtdYZKdmirYnn0bY9vKG:oIHj1cYFvKExvM{[zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU46PTF{IN88US=> MoPkV2FPT0WU
human NCI-H747 cell NXrFXZdxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mo\aTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEe0O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvODN|NUOg{txO MWDTRW5ITVJ?
human A498 cell NXjnOYdpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX;rRYpiUW6qaXLpeIlwdiCxZjDoeY1idiCDNEm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4{PjZ7IN88US=> MUfTRW5ITVJ?

... 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]
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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]
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  • 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

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