Midostaurin (PKC412)

For research use only.

Catalog No.S8064 Synonyms: CGP 41251

23 publications

Midostaurin (PKC412) Chemical Structure

CAS No. 120685-11-2

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 23 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 MnnFR5l1d3SxeHnjbZR6KGG|c3H5 MWS3NkBp MXPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNWlQuOTFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JINmdGxidHn0[ZIu[my3ZTDhd5NigSxiSVO1NF0yOiCwTR?= NFPuZnoyQTZ3NESwPC=>
RS4-11 cells NUfkPXFTTnWwY4Tpc44h[XO|YYm= MkK0NkBp MXrJcohq[mm2aX;uJI9nKE[OVEOgTXRFKG23dHHueEBifXSxcHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKFKVND2xNUBk\WyuczDh[pRmeiB{IHjyd{BjgSCnbHXjeJJw[2inbXnseY1qdmW|Y3XuZ4Uh[XO|YYmsJGlEPTB;MUOgcm0> MYixPVY2PDRyOB?=
CGTH-W-1 cell M4D3U2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MknGTY5pcWKrdHnvckBw\iCqdX3hckBET1SKLWetNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQzNjZ3IN88US=> NEfYbIxUSU6JRWK=
SW982 cell NWTES3NpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4HWZmlvcGmkaYTpc44hd2ZiaIXtZY4hW1d7OEKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20OU42QCEQvF2= MlTDV2FPT0WU
human EoL-1-cell cell MkjhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkPITY5pcWKrdHnvckBw\iCqdX3hckBGd0xvMT3j[YxtKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PTJwMEigcm0> NIjpRYlUSU6JRWK=
MOLM-13 cells MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3\6dlczKGh? MYrJcohq[mm2aX;uJI9nKE[OVEOgTXRFKGindHXyc5p6\2:3czDteZRidnRiaX6gbJVu[W5iTV;MUU0yOyClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGdKPTB;MD6wOVUh|ryP MXKyOlA5OTB{Mx?=
KASUMI-1 cell M2fvdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHLiTW1KdmirYnn0bY9vKG:oIHj1cYFvKEuDU2XNTU0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5yNkCxOkDPxE1? MX\TRW5ITVJ?
NCI-H1755 cell NEnXSpNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmLMTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG3OVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjB4MkezJO69VQ>? M1rqTXNCVkeHUh?=
human MES-SA cell NUfWenppT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHfEfJlKdmirYnn0bY9vKG:oIHj1cYFvKE2HUz3TRUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODd3NESg{txO NG\KO2pUSU6JRWK=
human HCC1395 cell NFPpcIZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkftTY5pcWKrdHnvckBw\iCqdX3hckBJS0NzM{m1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xQDR{ODFOwG0> MlPWV2FPT0WU
human D-336MG cell M3\n[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmDwTY5pcWKrdHnvckBw\iCqdX3hckBFNTN|Nl3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xQDd3NDFOwG0> MnW0V2FPT0WU
CHP-212 cell NHX3ZXpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkXGTY5pcWKrdHnvckBw\iCqdX3hckBEUFBvMkGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xQDd5MzFOwG0> MUTTRW5ITVJ?
human KM12 cell NGHjO5VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVXJcohq[mm2aX;uJI9nKGi3bXHuJGtOOTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkC5Nlc2KM7:TR?= M33ZOnNCVkeHUh?=
A204 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEDGb5RKdmirYnn0bY9vKG:oIHj1cYFvKEF{MESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlExODV{IN88US=> NFX6d41USU6JRWK=
CAL-51 cell M2TBVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnnqTY5pcWKrdHnvckBw\iCqdX3hckBESUxvNUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlExPzB7IN88US=> NIPzT3pUSU6JRWK=
human A431 cell MoXKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXzwV|JMUW6qaXLpeIlwdiCxZjDoeY1idiCDNEOxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yOTJzNjFOwG0> MlX0V2FPT0WU
NCI-H650 cell MnjJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlvaTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSE[1NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTF5MEig{txO NGP1WZVUSU6JRWK=
A427 cell M4L4S2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIrDfmhKdmirYnn0bY9vKG:oIHj1cYFvKEF2MkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEyQTF6IN88US=> MmH1V2FPT0WU
human 769-P cell M1vJcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF3lZnlKdmirYnn0bY9vKG:oIHj1cYFvKDd4OT3QJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yOjB6MjFOwG0> M3;NSnNCVkeHUh?=
SW1710 cell NYrTdFd2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVz3c5NNUW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF|M{G2JO69VQ>? MYHTRW5ITVJ?
human H4 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFj6c4hKdmirYnn0bY9vKG:oIHj1cYFvKEh2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xN|k3OyEQvF2= NFHJd5hUSU6JRWK=
HT-1080 cell NEWxWZBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{HBT2lvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMUC4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTV7OEKg{txO MWHTRW5ITVJ?
human PANC-03-27 cell NGjCTJpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWfxV5ZvUW6qaXLpeIlwdiCxZjDoeY1idiCSQV7DMVA{NTJ5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xOlAzKM7:TR?= M3HVe3NCVkeHUh?=
A375 cells NUX2XId5S3m2b4TvfIlkcXS7IHHzd4F6 MUO3NkBp M{K5OHRwgGmlaYT5JIFo[Wmwc4SgbJVu[W5iQUO3OUBk\WyuczDh[pRmeiB5MjDodpMh[nliY3XscEB1cXSncj3icJVmKGG|c3H5MEBKSzVyPUCuNVgh|ryP MWmxPVY2PDRyOB?=
human HOP-62 cell M{fwZ2Z2dmO2aX;uJIF{e2G7 Mlj5TY5pcWKrdHnvckBw\iCqdX3hckBJV1BvNkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE5ODd|IN88US=> NU\0VWlxW0GQR1XS
human U031 cell NYPBTYxMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXHJcohq[mm2aX;uJI9nKGi3bXHuJHUxOzFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG5Olk5KM7:TR?= NGPXdnNUSU6JRWK=
mouse BAF3 cells MkSxVJJwdGmoZYLheIlwdiCjc4PhfS=> MoLFRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCEQV[zJINmdGy|IITyZY5{\m:{bXXkJJdqfGhiWl7GNVk5NU[JRmKxJINwdnO2coXjeEwhUUN3ME2wMlIh|ryP NGnveHQzOTl|NkW0Ni=>
human G-402 cell NIC0[I9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGXCSW1KdmirYnn0bY9vKG:oIHj1cYFvKEdvNECyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zODJ3MzFOwG0> M3;sS3NCVkeHUh?=
human G-361 cell NIXROI9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUTJcohq[mm2aX;uJI9nKGi3bXHuJGcuOzZzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yNFg2OyEQvF2= NUjTcWpuW0GQR1XS
NCI-H810 cell NY[0WXBpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWrJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KOEGwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zOTB{NzFOwG0> NHTwS4hUSU6JRWK=
NCI-H2030 cell NITKfm1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX33Uo1{UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIxOzBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkKzNFA3KM7:TR?= MVrTRW5ITVJ?
human HCT-116 cell Ml\tS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1G0VWlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWLUGxOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjN3Nkig{txO Ml\FV2FPT0WU
human SNU-423 cell MkfSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlPKTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zOzZ3NzFOwG0> M{T3Z3NCVkeHUh?=
human SCC-4 cell NIKzXppIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWTJcohq[mm2aX;uJI9nKGi3bXHuJHNESy12IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yN|k3PyEQvF2= M{XsOnNCVkeHUh?=
human SW48 cell M4fIcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1HrXWlvcGmkaYTpc44hd2ZiaIXtZY4hW1d2ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlY3QCEQvF2= MWTTRW5ITVJ?
human SF295 cell M1W2ZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NY\uV|M1UW6qaXLpeIlwdiCxZjDoeY1idiCVRkK5OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjd{NUeg{txO NUP1[5JPW0GQR1XS
MDA-MB-231 cell M3r3Tmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUPJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2yN|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ6MUCxJO69VQ>? NWLaWXdGW0GQR1XS
A172 cell MlqzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUHqV5hQUW6qaXLpeIlwdiCxZjDoeY1idiCDMUeyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zQTF3IN88US=> NXfDS3p[W0GQR1XS
human BCPAP cell MnnES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2LtPGlvcGmkaYTpc44hd2ZiaIXtZY4hSkOSQWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI6QDd7IN88US=> M{fJcXNCVkeHUh?=
human COLO-792 cell M{fmNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vN{myJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zQTl5MjFOwG0> NW\MV4hUW0GQR1XS
human DU-145 cell Ml64S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWrXbm0{UW6qaXLpeIlwdiCxZjDoeY1idiCGVT2xOFUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjNzOEi5JO69VQ>? MVPTRW5ITVJ?
NCI-H2122 cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFTuUZVKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlEzOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{KyPFUh|ryP NHz3UWlUSU6JRWK=
human SK-UT-1 cell Mlf0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIrPPZNKdmirYnn0bY9vKG:oIHj1cYFvKFONLWXUMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN{OUWyJO69VQ>? MWnTRW5ITVJ?
LXF-289 cell M36zZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoT2TY5pcWKrdHnvckBw\iCqdX3hckBNYEZvMki5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{Ojl4NTFOwG0> M2G3UHNCVkeHUh?=
human NCI-H1792 cell NHO5[GZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mm[wTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG3PVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN|MEm2JO69VQ>? MUHTRW5ITVJ?
MCF7 cell M2HwVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn;UTY5pcWKrdHnvckBw\iCqdX3hckBOS0Z5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zN|I4PCEQvF2= MnT6V2FPT0WU
HCT-15 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4PqRWlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWLUG1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{OzR|MjFOwG0> NFTjN41USU6JRWK=
human NCI-H358 cell M1ftTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXLlR|BtUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFM2QCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{O1OVEh|ryP MVrTRW5ITVJ?
human HLE cell NXK2bVlTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFTWUIFKdmirYnn0bY9vKG:oIHj1cYFvKEiORTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|M4PTJizszN MoflV2FPT0WU
human SW1088 cell MoL5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3PCUGlvcGmkaYTpc44hd2ZiaIXtZY4hW1dzMEi4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{Ozd7NzFOwG0> MUnTRW5ITVJ?
human K5 cell NUTNOnpFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWXBVZozUW6qaXLpeIlwdiCxZjDoeY1idiCNNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|YyPDlizszN M{fVV3NCVkeHUh?=
human SR cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4O5bWlvcGmkaYTpc44hd2ZiaIXtZY4hW1JiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkO2OVcyKM7:TR?= NWHhPZI1W0GQR1XS
human Calu-3 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEfMU4JKdmirYnn0bY9vKG:oIHj1cYFvKEOjbIWtN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzZ6MkWg{txO MkjwV2FPT0WU
human SK-MEL-30 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NELENpFKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0{OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{m5NVMh|ryP NWqxdYtWW0GQR1XS
human SW780 cell M37wd2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGXy[YlKdmirYnn0bY9vKG:oIHj1cYFvKFOZN{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OTF2MjFOwG0> NVLiT4RKW0GQR1XS
NCI-H1563 cell NVHOSWpzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MonWTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG1OlMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjRzNEi0JO69VQ>? MY\TRW5ITVJ?
human MKN45 cell MnPTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIexb2tKdmirYnn0bY9vKG:oIHj1cYFvKE2NTkS1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OTl|MTFOwG0> NFrScppUSU6JRWK=
MDA-MB-157 cell NUPqbZN3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnvaTY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtNVU4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52MkCxOUDPxE1? M3;tbXNCVkeHUh?=
human NCI-H522 cell NYDpU|lNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIC4c|RKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IOVIzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52MkOg{txO NX6zU5RtW0GQR1XS
human A2780 cell NUHp[3hbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYjjSJpHUW6qaXLpeIlwdiCxZjDoeY1idiCDMke4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDd3MEOg{txO NWjzV|lEW0GQR1XS
human A498 cell NIjH[5pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NInlWFZKdmirYnn0bY9vKG:oIHj1cYFvKEF2OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ4Pjl|IN88US=> MnfmV2FPT0WU
human BxPC-3 cell NHjPSWNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH3MVlVKdmirYnn0bY9vKG:oIHj1cYFvKEK6UFOtN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDl|Nk[g{txO NVTCe3gxW0GQR1XS
human A2058 cell M17jZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3m4VGlvcGmkaYTpc44hd2ZiaIXtZY4hSTJyNUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlUzQDR2IN88US=> MkDoV2FPT0WU
human PC-14 cell M2DVbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYrJcohq[mm2aX;uJI9nKGi3bXHuJHBENTF2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD61N|g2PSEQvF2= NGO0fGFUSU6JRWK=
human KG-1 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2LFb2lvcGmkaYTpc44hd2ZiaIXtZY4hU0dvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOVU1OTlizszN NW\GO2xuW0GQR1XS
human A375 cell NFv3UWFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1\FdmlvcGmkaYTpc44hd2ZiaIXtZY4hSTN5NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOVYyODNizszN MlLsV2FPT0WU
human SW1783 cell NHHNcnhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYPJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTd6MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuO|M{PyEQvF2= MoXsV2FPT0WU
human MKN1 cell NULmW3RiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWX2OWhEUW6qaXLpeIlwdiCxZjDoeY1idiCPS16xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE45QDRzMjFOwG0> MUDTRW5ITVJ?
NCI-H1650 cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4ftRmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOlUxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC56OEmxOwOBiM7:TR?= M1;oTnNCVkeHUh?=
human HT-1376 cell Mo\1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2W4b2lvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMUO3OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvQTJ7MUig{txO Mne5V2FPT0WU
SW872 cell M2TuU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkDGTY5pcWKrdHnvckBw\iCqdX3hckBUXzh5MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuPVQ1PTlizszN MlLwV2FPT0WU
human RT-112 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVrFR4Y4UW6qaXLpeIlwdiCxZjDoeY1idiCUVD2xNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjl5NEizJO69VQ>? Mm\3V2FPT0WU
human HT-29 cell M3XxUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVfJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTJ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD65O|k6PiEQvF2= NUD0dIt7W0GQR1XS
human U-266 cell MlrDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGDSbHpKdmirYnn0bY9vKG:oIHj1cYFvKFVvMk[2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE46QDNyMjFOwG0> M3\IOnNCVkeHUh?=
human HEL cell M3zITGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmDqTY5pcWKrdHnvckBw\iCqdX3hckBJTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkm4OVE4KM7:TR?= Mn3JV2FPT0WU
human KU812 cell NF3iOopIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{fJSGlvcGmkaYTpc44hd2ZiaIXtZY4hU1V6MUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlEyOTZ2IN88US=> MYTTRW5ITVJ?

... 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 )

  • C1
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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):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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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