Midostaurin (PKC412)

Catalog No.S8064 Synonyms: CGP 41251

For research use only.

Midostaurin (pkc412, CGP 41251) is a multi-targeted kinase inhibitor, including PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50 ranging from 80-500 nM.

Midostaurin (PKC412) Chemical Structure

CAS No. 120685-11-2

Selleck's Midostaurin (PKC412) has been cited by 33 publications

Purity & Quality Control

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Biological Activity

Description Midostaurin (pkc412, CGP 41251) is a multi-targeted kinase inhibitor, including PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50 ranging from 80-500 nM.
Targets
PKCα [1]
(Cell-free assay)
PKCγ [1]
(Cell-free assay)
PKCβ1 [1]
(Cell-free assay)
PKCβ2 [1]
(Cell-free assay)
PPK [1]
(Cell-free assay)
Click to View More Targets
22 nM 24 nM 30 nM 31 nM 38 nM
In vitro

Midostaurin(pkc412) is a broad spectrum protein kinase inhibitor. Midostaurin(pkc412) interacts strongly with ATP binding sites of the conventional PKC-α, -β and -γ, PDGFRβ, VEGF-R2, VEGF-R1 and the cyclin-dependant kinase 1-cyclin B complex. Midostaurin(pkc412) inhibits the growth of various human and animal cell lines in vitro at similar submicromolar concentrations. Midostaurin(pkc412) also effectively inhibits the in vitro proliferation of glioblastoma and induced the accumulation of cells in G2/M and formation of giant nuclei with extensive fragmentation and apoptotic bodies. Midostaurin(pkc412) is able to reverse the p-glycoprotein-mediated multidrug resistance of tumor cells in vitro. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EOL-1 MYXDfZRwfG:6aXPpeJkh[XO|YYm= NFrld284OiCqcoO= M{TzWGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGVQVC1zIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFNiYYPzZZktKEmFNUCgQUAxNjByM{ig{txONg>? M1XYZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7M{WwPVIxLz5{OUO1NFkzODxxYU6=
MOLM13 M3nmdGN6fG:2b4jpZ4l1gSCjc4PhfS=> NF\jNFE4OiCqcoO= M{DpSWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1QVE1zMzDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCLQ{WwJF0hOC5yMES3JO69VS5? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTN3MEmyNEc,Ojl|NUC5NlA9N2F-
MV4-11 MUfDfZRwfG:6aXPpeJkh[XO|YYm= NX\MVHRKPzJiaILz NWfZ[WFoS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVVZ2LUGxJINmdGy|IHHmeIVzKDd{IHjyd{BjgSClZXzsJJRqfGW{LXLseYUh[XO|YYmsJGlEPTBiPTCwMlAyOiEQvF2u MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTZ3NESwPEc,OTl4NUS0NFg9N2F-
RS4-11 M4jmbGZ2dmO2aX;uJIF{e2G7 NGHJV|QzKGi{cx?= NITseWRKdmirYnn0bY9vKG:oIF\MWFMhUVSGIH31eIFvfCCjdYTvdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIGLTOE0yOSClZXzsd{Bi\nSncjCyJIhzeyCkeTDlcIVkfHKxY3jlcYltfW2rbnXzZ4Vv[2ViYYPzZZktKEmFNUCgQUAxNjBzMzFOwG0v M17jXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NkW0OFA5Lz5zOU[1OFQxQDxxYU6=
RS4-11 Mn7YSpVv[3Srb36gZZN{[Xl? NV\weXBHOiCqcoO= MX3Jcohq[mm2aX;uJI9nKE[OVEOgZZV1d3Cqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBTWzRvMUGgZ4VtdHNiYX\0[ZIhOiCqcoOgZpkh\WynY4Tyc4Np\W2rbIXtbY5me2OnbnPlJIF{e2G7LDDJR|UxKD1iMD6wNVUh|ryPLh?= NUXHR3pKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm2OVQ1ODhpPkG5OlU1PDB6PD;hQi=>
Sf9 MnnPSpVv[3Srb36gZZN{[Xl? MYW0JIhzew>? NGrEV2FKdmirYnn0bY9vKG:oIIfpcIQhfHmyZTDHV3QufGGpZ3XkJGZNXDNia3nuZZNmKGSxbXHpckApYTV4NzD0c{BUQTl|KTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CCrboPlZ5QhW2Z7IHPlcIx{KHW|aX7nJGhmejJicHXweIll\SCjczDzeYJ{fHKjdHWgZYZ1\XJiNDDodpMh[nliS3nuZZNmNUeubzDhd5NigSxiSVO1NEA:KDBwMEO3JO69VS5? M1XOO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEixNFI{Lz5{NkC4NVAzOzxxYU6=
MV4-11 NWnZdZdPTnWwY4Tpc44h[XO|YYm= M334PVczKGi{cx?= M{HoU2lvcGmkaYTpc44hd2ZiRlzUN{BKXERiaH;tc5p6\2:3czDteZRidnRiaX6gbJVu[W5iTW[0MVEyKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IECuNFM5KM7:TT6= M3TLbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEixNFI{Lz5{NkC4NVAzOzxxYU6=
MOLM-13 NFfofVdHfW6ldHnvckBie3OjeR?= MkPWO|IhcHK| MYTJcohq[mm2aX;uJI9nKE[OVEOgTXRFKGindHXyc5p6\2:3czDteZRidnRiaX6gbJVu[W5iTV;MUU0yOyClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGdKPTBiPTCwMlA2PSEQvF2u NX61NodzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFExOjNpPkK2NFgyODJ|PD;hQi=>
Sf9 M{TVb2Z2dmO2aX;uJIF{e2G7 NUTmdGh3QTBibXnudy=> MULJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IFfTWE11[WepZXSgRZVzd3KjLVGgb4lv[XOnIHTvcYFqdiBqU{GyN{B1dyCVNECxLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCrboPlZ5QhW2Z7IHPlcIx{KHW|aX7nJJRmfHKjKFzSVmFUVEdrIIDldJRq\GViYYOgd5Vje3S{YYTlJIFnfGW{IEmwJI1qdnNiYomgT4lv[XOnLVfsc{Bie3OjeTygTWM2OCB;IECuNFgh|ryPLh?= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MUCyN{c,OjZyOEGwNlM9N2F-
FDC-P1 NYC3cXJTTnWwY4Tpc44h[XO|YYm= NGLLZ|c1QCCqcoO= NFrYPFlKdmirYnn0bY9vKG:oIHj1cYFvKE[PUzDlfJBz\XO|ZXSgbY4h\3Kxd4ToJIZi[3SxcjDk[ZBmdmSnboSgcY92e2ViRlTDMXAyKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gSm1UNW2nZHnheIVlKGOnbHygdJJwdGmoZYLheIlwdiCrbjDwdoV{\W6lZTDoeY1idiCFU1[xJIFnfGW{IES4JIhzeyCkeTDy[ZNignW{aX6g[JlmKHKnZIXjeIlwdiCjc4PhfUwhUUN3MDC9JFAvOTR{IN88UU4> NGf2XYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEG1OlY5QSd-MkCxOVY3QDl:L3G+
A375 NUHkNYp6XG:6aXPpeJkh[XO|YYm= NFT0bY84OiCqcoO= NF3qTnpVd3irY3n0fUBi\2GrboP0JIh2dWGwIFGzO|Uh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IHPlcIwhfGm2ZYKtZox2\SCjc4PhfUwhUUN3MDC9JFAvOThizszNMi=> NHvoWGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOU[1OFQxQCd-MUm2OVQ1ODh:L3G+
FDC-P1 NIjke3VHfW6ldHnvckBie3OjeR?= NXXldHlXPDhiaILz MnrpTY5pcWKrdHnvckBw\iCvb4Xz[UBIVS2FU1[td5RqdXWuYYTl[EBk\WyuIIDyc4xq\mW{YYTpc44hd2ZiZ4Lve5RpKG[jY4TvdkBl\XCnbnTlcpQhdW:3c3WgSmRENVBzIHPlcIx{KGW6cILld5NqdmdiaIXtZY4hTk2VIHHmeIVzKDR6IHjyd{BjgSC{ZYPhfpVzcW5iZInlJJJm\HWldHnvckBie3OjeTygTWM2OCB;IECuNkDPxE1w NGjiZ5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEG1OlY5QSd-MkCxOVY3QDl:L3G+
BAF3 M{HwVGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M{G2c2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViQlHGN{Bk\WyuczD0doFve2[xcn3l[EB4cXSqIGrOSlE6QC2IR1\SNUBkd26|dIL1Z5QtKEmFNUCgQUAxNjJizszNMi=> MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl|NkW0Nkc,OjF7M{[1OFI9N2F-
Sf9 NV3ZXWg2TnWwY4Tpc44h[XO|YYm= MkDKNVIxKG2rboO= NXHJVFczUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBIW1RvdHHn[4VlKF[HR1\SNkBscW6jc3Wg[I9u[WmwIDjWO|g6KHSxIG[xN|U3MSBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDpcpNm[3RiU3[5JINmdGy|IIXzbY5oKHCxbInHcJU1QlS7cjDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBi\nSncjCxNlAhdWmwczDifUBMcW6jc3WtS4xwKGG|c3H5MEBKSzVyIE2gNE4zPSEQvF2u M3XQdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEixNFI{Lz5{NkC4NVAzOzxxYU6=
RS4:11 NHK1fnZHfW6ldHnvckBie3OjeR?= MoPmO|IhcHK| MUXJcohq[mm2aX;uJI9nKHerbHSgeJlx\SCqb33vfplod3W|IF\MWFMhcW5iaIXtZY4hWlN2OkGxJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiR1m1NEA:KDBwNDFOwG0v M4XG[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEixNFI{Lz5{NkC4NVAzOzxxYU6=
U937 M2fVb2N6fG:2b4jpZ4l1gSCjc4PhfS=> NIG4eoE4OiCqcoO= NHfD[JdEgXSxdH;4bYNqfHliYXfhbY5{fCCITGSzMYRm\mmlaXXueEBpfW2jbjDVPVM4KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IEGuOEDPxE1w MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MUCyN{c,OjZyOEGwNlM9N2F-
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SK-N-MC NIC4PVVyUFSVIHHzd4F6 NWLtNVZPeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> M1\CNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
U-2 OS M2DHXZFJXFNiYYPzZZk> MXHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhXS1{IF;TJINmdGy| M2\EWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Saos-2 M3nVfZFJXFNiYYPzZZk> MUfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| MnraQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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LAN-5 NX\VSXdjeUiWUzDhd5NigQ>? MmnRdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| MoT6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh18 MVfxTHRUKGG|c3H5 MYrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmhzODDj[Yxtew>? NYfYfVJnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 M{PyXZFJXFNiYYPzZZk> M2LBPZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO= NXvGfWdSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R) MlrGdWhVWyCjc4PhfS=> MV;xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? MmLwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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OVCAR-8 NVr6[GF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVWyUIFlUW6qaXLpeIlwdiCxZjDoeY1idiCRVlPBVk05KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB{LkCzNVUh|ryPLh?= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly2NFg2OzNxJ{7TRW5ITVJ:L3G+
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Calu-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;uTWZjUW6qaXLpeIlwdiCxZjDoeY1idiCFYXz1MVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDJwMUK0NFUh|ryPLh?= MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly2NFg2OzNxJ{7TRW5ITVJ:L3G+
LC-1F M1rsNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfIbphKdmirYnn0bY9vKG:oIHj1cYFvKEyFLUHGJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAzNjF2N{[0JO69VS5? NVfR[HZKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPjB6NUOzM{c,W0GQR1XSQE9iRg>?
NEC8 NFfJSYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{KycWlvcGmkaYTpc44hd2ZiaIXtZY4hVkWFODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNk4yPTZyMTFOwG0v NHPwPGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw3ODh3M{OvK|5USU6JRWK8M4E,
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BHT-101 M3\5cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLGTY5pcWKrdHnvckBw\iCqdX3hckBDUFRvMUCxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAzNjF7NkW0JO69VS5? M3G4OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFYxQDV|Mz:nQnNCVkeHUkyvZV4>
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CAPAN-1 M1TJdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3SSYt[UW6qaXLpeIlwdiCxZjDoeY1idiCFQWDBUk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB{LkK0O|g4KM7:TT6= MnPmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOlA5PTN|Lze+V2FPT0WUPD;hQi=>
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NCI-H1304 NIrOOZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFqzZ4NKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVMxPCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iMj6yPFg3PyEQvF2u NEHDflg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw3ODh3M{OvK|5USU6JRWK8M4E,
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KINGS-1 M1TG[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGntNYZKdmirYnn0bY9vKG:oIHj1cYFvKEuLTlfTMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDJwM{CyO|Eh|ryPLh?= NHfJbXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw3ODh3M{OvK|5USU6JRWK8M4E,
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UACC-893 M3G5d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTlTY5pcWKrdHnvckBw\iCqdX3hckBWSUOFLUi5N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hPDdwM{ezOkDPxE1w NIGxUHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw3ODh3M{OvK|5USU6JRWK8M4E,
Assay
Methods Test Index PMID
Western blot PKCα / PKCβ1 / PKCβ2 / PKCγ / PKCη / p-PKC / p-Bad / Bad / p-Bcl2 / Bcl-2 / p-p65 / p65 ; p-TYR / p-STAT5 / STAT5 / p-S6 / S6 / p-MAPK / MAPK / p-AKT / AKT 30584254 28881711
In vivo Midostaurin(pkc412) may suppress tumor growth by inhibiting tumor angiogenesis (via its effects on the VEGF receptor tyrosine kinases) in addition to directly inhibiting tumor cell proliferation (via its effects on PKCs). This anti-angiogenic action may contribute to the antimetastatic and broad antitumor activity displayed by midostaurin(pkc412), as well as the synergy with cytotoxic agents, including doxorubicin, cyclophosphamide, cisplatin and gemcitabine. When given orally, the maximally tolerated dose for midostaurin(pkc412) is >300 mg/kg. [1]

Protocol (from reference)

Cell Research:[2]
  • Cell lines: A549, NCI-H520
  • Concentrations: ~1.0 μM
  • Incubation Time: 24-72 h
  • Method: Each well is added with 5 mM WST-1 and 0.2 mM 1-methoxy PMS and the absorbance at 450 nm is measured by a Microplate Reader.
Animal Research:[1]
  • Animal Models: Colo 205 colorectal tumors xenograft
  • Dosages: 50 mg/kg, 200 mg/kg, once daily
  • Administration: p.o.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+45% PEG 300+ddH2O
For best results, use promptly after mixing.

4mg/mL

Chemical Information

Molecular Weight 570.64
Formula

C35H30N4O4

CAS No. 120685-11-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC12C(C(CC(O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)N(C)C(=O)C9=CC=CC=C9)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03951961 Terminated Drug: Midostaurin Acute Myeloid Leukemia Adult University of Jena|Ludwig-Maximilians - University of Munich March 20 2020 Phase 2
NCT04097470 Active not recruiting Drug: Decitabine|Drug: Midostaurin AML/MDS Stichting Hemato-Oncologie voor Volwassenen Nederland|Swiss Group for Clinical Cancer Research December 5 2019 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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

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