Midostaurin (PKC412)

For research use only.

Catalog No.S8064 Synonyms: CGP 41251

20 publications

Midostaurin (PKC412) Chemical Structure

Molecular Weight(MW): 570.64

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.

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Selleck's Midostaurin (PKC412) has been cited by 20 publications

Purity & Quality Control

Choose Selective PKC Inhibitors

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)
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
human MV4-11 cells MnzGR5l1d3SxeHnjbZR6KGG|c3H5 MmHXO|IhcA>? MWXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNWlQuOTFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JINmdGxidHn0[ZIu[my3ZTDhd5NigSxiSVO1NF0yOiCwTR?= Mk\FNVk3PTR2MEi=
RS4-11 cells NWnpZVY6TnWwY4Tpc44h[XO|YYm= MWSyJIg> Mn20TY5pcWKrdHnvckBw\iCITGSzJGlVTCCvdYThcpQh[XW2b4Doc5NxcG:{eXzheIlwdiCrbjDoeY1idiCUU{StNVEh[2WubIOgZYZ1\XJiMjDodpMh[nliZXzlZ5Rzd2OqZX3pcJVucW6nc3PlcoNmKGG|c3H5MEBKSzVyPUGzJI5O M4LKeFE6PjV2NEC4
CGTH-W-1 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4nuRWlvcGmkaYTpc44hd2ZiaIXtZY4hS0eWSD3XMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Oi54NTFOwG0> NFvtVFNUSU6JRWK=
SW982 cell NEDrUmRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVj3NXZPUW6qaXLpeIlwdiCxZjDoeY1idiCVV{m4NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ2NjV6IN88US=> MV;TRW5ITVJ?
human EoL-1-cell cell MnLFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnLJTY5pcWKrdHnvckBw\iCqdX3hckBGd0xvMT3j[YxtKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PTJwMEigcm0> MW\TRW5ITVJ?
MOLM-13 cells MnHtS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml\SO|IhcA>? NXPQNXZXUW6qaXLpeIlwdiCxZjDGUHQ{KEmWRDDo[ZRmem:8eXfveZMhdXW2YX70JIlvKGi3bXHuJG1QVE1vMUOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCJSUWwQVAvODV3IN88US=> MkPaNlYxQDFyMkO=
KASUMI-1 cell MmnkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmToTY5pcWKrdHnvckBw\iCqdX3hckBMSVOXTVmtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODZyMU[g{txO M{jiUnNCVkeHUh?=
NCI-H1755 cell M4HkTWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYHJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUe1OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODZ{N{Og{txO NFHMXYdUSU6JRWK=
human MES-SA cell NUn1[|dFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MU\Jcohq[mm2aX;uJI9nKGi3bXHuJG1GWy2VQTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFc2PDRizszN MknlV2FPT0WU
human HCC1395 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkXDTY5pcWKrdHnvckBw\iCqdX3hckBJS0NzM{m1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xQDR{ODFOwG0> MWrTRW5ITVJ?
human D-336MG cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmrLTY5pcWKrdHnvckBw\iCqdX3hckBFNTN|Nl3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xQDd3NDFOwG0> NXntSm5yW0GQR1XS
CHP-212 cell M4rx[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmHETY5pcWKrdHnvckBw\iCqdX3hckBEUFBvMkGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xQDd5MzFOwG0> NUP1N2pRW0GQR1XS
human KM12 cell M2f3NWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVTJcohq[mm2aX;uJI9nKGi3bXHuJGtOOTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkC5Nlc2KM7:TR?= NXv4VJhPW0GQR1XS
A204 cell NE\DdWRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXvCbndJUW6qaXLpeIlwdiCxZjDoeY1idiCDMkC0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yODB3MjFOwG0> MY\TRW5ITVJ?
CAL-51 cell MorKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4fRNWlvcGmkaYTpc44hd2ZiaIXtZY4hS0GOLUWxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yODdyOTFOwG0> Mmn1V2FPT0WU
human A431 cell NHj2doJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlLPTY5pcWKrdHnvckBw\iCqdX3hckBCPDNzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xNVIyPiEQvF2= MX3TRW5ITVJ?
NCI-H650 cell MoHES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3\hV2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi2OVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjFzN{C4JO69VQ>? NVfMdpFWW0GQR1XS
A427 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVHFV4VoUW6qaXLpeIlwdiCxZjDoeY1idiCDNEK3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yOTlzODFOwG0> NHTuNmFUSU6JRWK=
human 769-P cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MljCTY5pcWKrdHnvckBw\iCqdX3hckA4PjlvUDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVIxQDJizszN NWnyZmU6W0GQR1XS
SW1710 cell MmK1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFX3O2tKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTN|MU[g{txO NFjjVIZUSU6JRWK=
human H4 cell NGDITYxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYrJcohq[mm2aX;uJI9nKGi3bXHuJGg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zM{m2N{DPxE1? NI[yd3lUSU6JRWK=
HT-1080 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVvJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTFyOECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE2QTh{IN88US=> MV;TRW5ITVJ?
human PANC-03-27 cell NGH6XYxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUXJcohq[mm2aX;uJI9nKGi3bXHuJHBCVkNvMEOtNlch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF4MEKg{txO NUT1WZhiW0GQR1XS
A375 cells MWLDfZRwfG:6aXPpeJkh[XO|YYm= MXi3NkBp MkfIWI95cWOrdImgZYdicW6|dDDoeY1idiCDM{e1JINmdGy|IHHmeIVzKDd{IHjyd{BjgSClZXzsJJRqfGW{LXLseYUh[XO|YYmsJGlEPTB;MD6xPEDPxE1? NWHUb3hyOTl4NUS0NFg>
human HOP-62 cell M1rmUmZ2dmO2aX;uJIF{e2G7 NXnkU4FkUW6qaXLpeIlwdiCxZjDoeY1idiCKT2CtOlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF6MEezJO69VQ>? M3TiUXNCVkeHUh?=
human U031 cell M4LPWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWSzelF1UW6qaXLpeIlwdiCxZjDoeY1idiCXMEOxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yQTZ7ODFOwG0> M{C1XHNCVkeHUh?=
mouse BAF3 cells MXvQdo9tcW[ncnH0bY9vKGG|c3H5 Mm\1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCEQV[zJINmdGy|IITyZY5{\m:{bXXkJJdqfGhiWl7GNVk5NU[JRmKxJINwdnO2coXjeEwhUUN3ME2wMlIh|ryP NGHOVnozOTl|NkW0Ni=>
human G-402 cell NHXPbWRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEXJZVFKdmirYnn0bY9vKG:oIHj1cYFvKEdvNECyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zODJ3MzFOwG0> NXzMcG9MW0GQR1XS
human G-361 cell NGPxOINIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3vGU2lvcGmkaYTpc44hd2ZiaIXtZY4hTy1|NkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIxQDV|IN88US=> MoX2V2FPT0WU
NCI-H810 cell NV20XWhIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHrCVZFKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IPFExKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{MUCyO{DPxE1? NVPBOFVSW0GQR1XS
NCI-H2030 cell M1zCTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkXQTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKwN|Ah[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ|MEC2JO69VQ>? MYLTRW5ITVJ?
human HCT-116 cell M2nDT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M37tS2lvcGmkaYTpc44hd2ZiaIXtZY4hUEOWLUGxOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjN3Nkig{txO NWn6cHFkW0GQR1XS
human SNU-423 cell MoPWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1GwfWlvcGmkaYTpc44hd2ZiaIXtZY4hW06XLUSyN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjN4NUeg{txO NX7nRlR7W0GQR1XS
human SCC-4 cell NYHacZlST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2\sR2lvcGmkaYTpc44hd2ZiaIXtZY4hW0OFLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI{QTZ5IN88US=> M4\4OnNCVkeHUh?=
human SW48 cell MnvXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3fqO2lvcGmkaYTpc44hd2ZiaIXtZY4hW1d2ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlY3QCEQvF2= NXGwU4FSW0GQR1XS
human SF295 cell NEHTPG9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYfJcohq[mm2aX;uJI9nKGi3bXHuJHNHOjl3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yO|I2PyEQvF2= MoH4V2FPT0WU
MDA-MB-231 cell NETMVYJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXfJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2yN|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ6MUCxJO69VQ>? M4PPcHNCVkeHUh?=
A172 cell M4PtO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mo\GTY5pcWKrdHnvckBw\iCqdX3hckBCOTd{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yPVE2KM7:TR?= M2fld3NCVkeHUh?=
human BCPAP cell NX\wfZFiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoH2TY5pcWKrdHnvckBw\iCqdX3hckBDS1CDUDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlk5PzlizszN M1vE[nNCVkeHUh?=
human COLO-792 cell NE\XfpZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYXpRmtFUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVc6OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMkm5O|Ih|ryP NGLLVplUSU6JRWK=
human DU-145 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2rB[GlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvMUS1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{OTh6OTFOwG0> NWLDWnpIW0GQR1XS
NCI-H2122 cell NIDOTYZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1;rWGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNVIzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|MkK4OUDPxE1? NXfkV4JlW0GQR1XS
human SK-UT-1 cell NGPCNFVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnnZTY5pcWKrdHnvckBw\iCqdX3hckBUUy2XVD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{Ojl3MjFOwG0> M37xO3NCVkeHUh?=
LXF-289 cell NV[0PIlzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnLYTY5pcWKrdHnvckBw\iCqdX3hckBNYEZvMki5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{Ojl4NTFOwG0> M3LyWHNCVkeHUh?=
human NCI-H1792 cell MmH4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3jwU2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixO|kzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|M{C5OkDPxE1? MYXTRW5ITVJ?
MCF7 cell NX;EeXhJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmXNTY5pcWKrdHnvckBw\iCqdX3hckBOS0Z5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zN|I4PCEQvF2= MWrTRW5ITVJ?
HCT-15 cell NUDtb2NWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUnufmlCUW6qaXLpeIlwdiCxZjDoeY1idiCKQ2StNVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN|NEOyJO69VQ>? NFOwe5lUSU6JRWK=
human NCI-H358 cell Mlf0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFu5XnVKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IN|U5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|M{W1NUDPxE1? M1XyV3NCVkeHUh?=
human HLE cell NILZOIZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2fzS2lvcGmkaYTpc44hd2ZiaIXtZY4hUEyHIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zN|c2OiEQvF2= NHvtbmRUSU6JRWK=
human SW1088 cell M3TVeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWrJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTB6ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|M4QTdizszN MXLTRW5ITVJ?
human K5 cell NETjU2FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2rmRmlvcGmkaYTpc44hd2ZiaIXtZY4hUzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkO2NVQ6KM7:TR?= M3HIU3NCVkeHUh?=
human SR cell MlvZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYXTdHdbUW6qaXLpeIlwdiCxZjDoeY1idiCVUjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|Y2PzFizszN NGTGXnlUSU6JRWK=
human Calu-3 cell MmTnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlTLTY5pcWKrdHnvckBw\iCqdX3hckBE[Wy3LUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM3QDJ3IN88US=> NFjkdWZUSU6JRWK=
human SK-MEL-30 cell M1:4dGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmfhTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytN|Ah[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN7OUGzJO69VQ>? M3XvfXNCVkeHUh?=
human SW780 cell M3rVZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M17pNGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d5OECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQyOTR{IN88US=> Mnz0V2FPT0WU
NCI-H1563 cell NVK1RYI6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXj6XphmUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE2PjNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkSxOFg1KM7:TR?= NVHMPIhlW0GQR1XS
human MKN45 cell NUfnOGs5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFj3XXpKdmirYnn0bY9vKG:oIHj1cYFvKE2NTkS1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OTl|MTFOwG0> NWXTNllQW0GQR1XS
MDA-MB-157 cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWTaOHNZUW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuOTV5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60NlAyPSEQvF2= MULTRW5ITVJ?
human NCI-H522 cell MoPLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVnJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KNUKyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OjNizszN M{PucXNCVkeHUh?=
human A2780 cell NHr6OGNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIDZN5ZKdmirYnn0bY9vKG:oIHj1cYFvKEF{N{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41PzVyMzFOwG0> Ml:1V2FPT0WU
human A498 cell NFHIN4RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGPvTZFKdmirYnn0bY9vKG:oIHj1cYFvKEF2OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ4Pjl|IN88US=> MYjTRW5ITVJ?
human BxPC-3 cell MoLQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4q1[GlvcGmkaYTpc44hd2ZiaIXtZY4hSniSQz2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41QTN4NjFOwG0> M1\pUHNCVkeHUh?=
human A2058 cell M2q5[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{XLfmlvcGmkaYTpc44hd2ZiaIXtZY4hSTJyNUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlUzQDR2IN88US=> NYG5ZWtbW0GQR1XS
human PC-14 cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXvQZ4hGUW6qaXLpeIlwdiCxZjDoeY1idiCSQz2xOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTN6NUWg{txO M33EVXNCVkeHUh?=
human KG-1 cell NWf6S49NT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MY\Jcohq[mm2aX;uJI9nKGi3bXHuJGtINTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkW1OFE6KM7:TR?= MVXTRW5ITVJ?
human A375 cell MniwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWjJcohq[mm2aX;uJI9nKGi3bXHuJGE{PzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkW2NVA{KM7:TR?= MXjTRW5ITVJ?
human SW1783 cell NHWxPVdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnrqTY5pcWKrdHnvckBw\iCqdX3hckBUXzF5OEOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlc{OzdizszN MmLkV2FPT0WU
human MKN1 cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlHMTY5pcWKrdHnvckBw\iCqdX3hckBOU05zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD64PFQyOiEQvF2= NVjNO41qW0GQR1XS
NCI-H1650 cell NVm1S2dIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGXlXWNKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVY2OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwOEi5NVbkiIEQvF2= M3jmU3NCVkeHUh?=
human HT-1376 cell M1fkeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2Xic2lvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMUO3OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvQTJ7MUig{txO M2XyfnNCVkeHUh?=
SW872 cell M13hemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEjLdIZKdmirYnn0bY9vKG:oIHj1cYFvKFOZOEeyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE46PDR3OTFOwG0> MnjyV2FPT0WU
human RT-112 cell NVvTS2xiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYrEVWhpUW6qaXLpeIlwdiCxZjDoeY1idiCUVD2xNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjl5NEizJO69VQ>? MnzPV2FPT0WU
human HT-29 cell NGTOSJlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4PXZWlvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlk4QTl4IN88US=> Ml;CV2FPT0WU
human U-266 cell MonPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{jUbmlvcGmkaYTpc44hd2ZiaIXtZY4hXS1{Nk[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlk5OzB{IN88US=> MoS0V2FPT0WU
human HEL cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGhGVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwOUi1NVch|ryP MYTTRW5ITVJ?
human KU812 cell M{XFRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHOyRolKdmirYnn0bY9vKG:oIHj1cYFvKEuXOEGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4yOTF4NDFOwG0> NVLUOph5W0GQR1XS

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-TYR / p-STAT5 / STAT5 / p-S6 / S6 / p-MAPK / MAPK / p-AKT / AKT ; 

PubMed: 28881711     


Effect of midostaurin and PRT062607 on TEL-SYK phosphorylation and phosphorylation of downstream effectors following 2 hr of treatment. For the experiment analyzing effects of midostaurin and PRT062607 on phosphorylation of TEL-SYK, SYK immunoprecipitation was carried out prior to immunoblotting with a PTYR (4G10) antibody. Immunoblotting was performed for the experiment analyzing effects of midostaurin and PRT062607 on signaling molecules downstream of TEL-SYK. Relative densitometry readings for pMAPK/total MAPK (normalized to control lane) are as follows: 0 nM midostaurin=1.0, 10 nM midostaurin=0.93, 100 nM midostaurin=0.41, 1000 nM midostaurin=0.04, 0 nM PRT062607=1.0, 10 nM PRT062607=0.72, 100 nM PRT062607=0.37, 1000 nM PRT062607=0.07. 

PKCα / PKCβ1 / PKCβ2 / PKCγ / PKCη / p-PKC / p-Bad / Bad / p-Bcl2 / Bcl-2 / p-p65 / p65; 

PubMed: 30584254     


The indicated PKC isoforms were up-regulated in the resistant BL cells, leading to elevated levels of PKC phosphorylation and the activation of downstream anti-apoptotic proteins.

28881711 30584254
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

Cell Research:[2]
- Collapse
  • 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.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: Colo 205 colorectal tumors xenograft
  • Dosages: 50 mg/kg, 200 mg/kg, once daily
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (175.24 mM)
Water Insoluble
Ethanol '20 mg/mL warmed
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

* 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 570.64
Formula

C35H30N4O4

CAS No. 120685-11-2
Storage powder
in solvent
Synonyms CGP 41251
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)
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)

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*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 )

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* 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):
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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

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03951961 Not yet recruiting Drug: Midostaurin Acute Myeloid Leukemia Adult Sebastian Scholl PD Dr. med.|Ludwig-Maximilians - University of Munich|University of Jena May 1 2020 Phase 2
NCT04097470 Recruiting Drug: Decitabine|Drug: Midostaurin AML/MDS Stichting Hemato-Oncologie voor Volwassenen Nederland|Swiss Group for Clinical Cancer Research December 5 2019 Phase 2

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.

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PKC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID