Midostaurin (PKC412)

Catalog No.S8064 Synonyms: CGP 41251

Midostaurin (PKC412) Chemical Structure

Molecular Weight(MW): 570.64

Midostaurin (pkc412) 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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Cited by 8 Publications

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  • (f and g) Induction of apoptosis in HMC-1.1 and -1.2, respectively. Columns represent the mean of three independent experiments and the bars represent the standard error. ctrl, control; mido, midostaurin.

    Leukemia, 2018, 32(1):139-148. Midostaurin (PKC412) purchased from Selleck.

    PKC412 is cytotoxic to human HNSCC cells. The established HNSCC cells (SQ20B and SCC‐9 cell lines), primary human oral carcinoma cells (“Primary1/2”) and primary oral epithelial cells (“Epithelial”), were treated with indicated concentrations of PKC412. Cells were then cultured in complete medium for the applied time, and cell survival was tested by the MTT assay (a, d) and colony formation assay (c). Cell death was tested by the trypan blue staining assay (b). “CTR” indicates medium‐treated control group (for all figures). All the experiments were repeated five times, and similar results were obtained. n = 5 for each assay. Error bars indicate mean ± SD (for all figures). *p < 0.05 versus group “CTR.” HNSCC, head and neck squamous cell carcinoma; MTT, 3‐(4,5‐dimethyl‐thiazol-2-yl)2,5-diphenyl tetrazolium bromide; OD, optical density; PKC, protein kinase C

    J Cell Physiol, 2018, 233(12):9437-9446. Midostaurin (PKC412) purchased from Selleck.

Purity & Quality Control

Choose Selective PKC Inhibitors

Biological Activity

Description Midostaurin (pkc412) 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 NWXFSnNwS3m2b4TvfIlkcXS7IHHzd4F6 M{DZelczKGh? NYDaOJA2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVVZ2LUGxJINmdGy|IHHmeIVzKDd{IHjyd{BjgSClZXzsJJRqfGW{LXLseYUh[XO|YYmsJGlEPTB;MUKgcm0> M4jCO|E6PjV2NEC4
RS4-11 cells NXi2OGFLTnWwY4Tpc44h[XO|YYm= MlfWNkBp M3PDXGlvcGmkaYTpc44hd2ZiRlzUN{BKXERibYX0ZY51KGG3dH;wbI9{eGixconsZZRqd25iaX6gbJVu[W5iUmO0MVEyKGOnbHzzJIFnfGW{IEKgbJJ{KGK7IHXs[YN1em:laHXtbYx2dWmwZYPj[Y5k\SCjc4PhfUwhUUN3ME2xN{BvVQ>? NXjvVINzOTl4NUS0NFg>
CGTH-W-1 cell M3zKdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWjJcohq[mm2aX;uJI9nKGi3bXHuJGNIXEhvVz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFIvPjVizszN NHKybXRUSU6JRWK=
SW982 cell MkXtS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGntRnlKdmirYnn0bY9vKG:oIHj1cYFvKFOZOUiyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFUvPThizszN NIHNeFZUSU6JRWK=
human EoL-1-cell cell NHHJZY5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVTrO2E2UW6qaXLpeIlwdiCxZjDoeY1idiCHb1ytNU1k\WyuIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUKuNFghdk1? NF;6TIJUSU6JRWK=
MOLM-13 cells MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnXuO|IhcA>? NGD0botKdmirYnn0bY9vKG:oIF\MWFMhUVSGIHjleIVzd3q7Z3;1d{BufXSjboSgbY4hcHWvYX6gUW9NVS1zMzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFczKGi{czDifUBOXFNiYYPzZZktKEeLNUC9NE4xPTVizszN NVjxVmpCOjZyOEGwNlM>
KASUMI-1 cell M3P3cWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV3kOmJOUW6qaXLpeIlwdiCxZjDoeY1idiCNQWPVUWkuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwME[wNVYh|ryP NV7lN481W0GQR1XS
NCI-H1755 cell MlTVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3r5cWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixO|U2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5yNkK3N{DPxE1? NVznbYh3W0GQR1XS
human MES-SA cell NGDPXJZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3X0e2lvcGmkaYTpc44hd2ZiaIXtZY4hVUWVLWPBJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xPzV2NDFOwG0> NFuwfHlUSU6JRWK=
human HCC1395 cell M{faOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnOxTY5pcWKrdHnvckBw\iCqdX3hckBJS0NzM{m1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xQDR{ODFOwG0> MlLnV2FPT0WU
human D-336MG cell NXTQ[opvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3fUXGlvcGmkaYTpc44hd2ZiaIXtZY4hTC1|M{\NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODh5NUSg{txO NHHZb|dUSU6JRWK=
CHP-212 cell MonUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHjJTndKdmirYnn0bY9vKG:oIHj1cYFvKEOKUD2yNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjB6N{ezJO69VQ>? MVXTRW5ITVJ?
human KM12 cell NUHkd5cxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYnuTIppUW6qaXLpeIlwdiCxZjDoeY1idiCNTUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xQTJ5NTFOwG0> MX\TRW5ITVJ?
A204 cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1K3Z2lvcGmkaYTpc44hd2ZiaIXtZY4hSTJyNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVAxPTJizszN NUHCSWhTW0GQR1XS
CAL-51 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYm5TVBSUW6qaXLpeIlwdiCxZjDoeY1idiCFQVytOVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjFyN{C5JO69VQ>? M36ySHNCVkeHUh?=
human A431 cell M2jwRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX;6SZVsUW6qaXLpeIlwdiCxZjDoeY1idiCDNEOxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yOTJzNjFOwG0> MUTTRW5ITVJ?
NCI-H650 cell M2q0[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmjuTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSE[1NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTF5MEig{txO M4LTNnNCVkeHUh?=
A427 cell Ml\YS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MW\Jcohq[mm2aX;uJI9nKGi3bXHuJGE1OjdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGxPVE5KM7:TR?= NWjJRXg5W0GQR1XS
human 769-P cell M4\hOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmHvTY5pcWKrdHnvckBw\iCqdX3hckA4PjlvUDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVIxQDJizszN NH\j[5NUSU6JRWK=
SW1710 cell MmXkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX60VZNPUW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF|M{G2JO69VQ>? NH:zdYNUSU6JRWK=
human H4 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1ewTGlvcGmkaYTpc44hd2ZiaIXtZY4hUDRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGzPVY{KM7:TR?= MUHTRW5ITVJ?
HT-1080 cell Mlm4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUXJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTFyOECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE2QTh{IN88US=> MlPvV2FPT0WU
human PANC-03-27 cell NVXqcJYzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXHofWl2UW6qaXLpeIlwdiCxZjDoeY1idiCSQV7DMVA{NTJ5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xOlAzKM7:TR?= NYTF[nY5W0GQR1XS
A375 cells MmjqR5l1d3SxeHnjbZR6KGG|c3H5 MXS3NkBp NY\2[mw4XG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBN|c2KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYJtfWViYYPzZZktKEmFNUC9NE4yQCEQvF2= MYixPVY2PDRyOB?=
human HOP-62 cell NELxRplHfW6ldHnvckBie3OjeR?= NW\ycItVUW6qaXLpeIlwdiCxZjDoeY1idiCKT2CtOlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF6MEezJO69VQ>? MlHvV2FPT0WU
human U031 cell NEXvPHNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1HXc2lvcGmkaYTpc44hd2ZiaIXtZY4hXTB|MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVk3QThizszN M{PuV3NCVkeHUh?=
mouse BAF3 cells NGnWfI1Rem:uaX\ldoF1cW:wIHHzd4F6 MnfhRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCEQV[zJINmdGy|IITyZY5{\m:{bXXkJJdqfGhiWl7GNVk5NU[JRmKxJINwdnO2coXjeEwhUUN3ME2wMlIh|ryP MUCyNVk{PjV2Mh?=
human G-402 cell NIi0e5BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmLGTY5pcWKrdHnvckBw\iCqdX3hckBINTRyMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlAzPTNizszN Mn3wV2FPT0WU
human G-361 cell NHrSXXBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MofqTY5pcWKrdHnvckBw\iCqdX3hckBINTN4MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlA5PTNizszN MXHTRW5ITVJ?
NCI-H810 cell MoTsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXfHcHBJUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFgyOCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMkGwNlch|ryP M2XrSHNCVkeHUh?=
NCI-H2030 cell NVnabZRKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX73cmdvUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIxOzBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkKzNFA3KM7:TR?= MnXlV2FPT0WU
human HCT-116 cell Mlv2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnjPTY5pcWKrdHnvckBw\iCqdX3hckBJS1RvMUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zOzV4ODFOwG0> NVL3WIU3W0GQR1XS
human SNU-423 cell NEXhRWZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFXkbIRKdmirYnn0bY9vKG:oIHj1cYFvKFOQVT20NlMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ|NkW3JO69VQ>? NI[wVFhUSU6JRWK=
human SCC-4 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVi0RpVlUW6qaXLpeIlwdiCxZjDoeY1idiCVQ1OtOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjN7Nkeg{txO MUjTRW5ITVJ?
human SW48 cell NYG1bZJQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHm2bY5KdmirYnn0bY9vKG:oIHj1cYFvKFOZNEigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI3PjhizszN M2O5T3NCVkeHUh?=
human SF295 cell M1frPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MofVTY5pcWKrdHnvckBw\iCqdX3hckBUTjJ7NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlczPTdizszN NYDHcHo6W0GQR1XS
MDA-MB-231 cell NWfCNFdwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1fhb2lvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVI{OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMkixNFEh|ryP MWjTRW5ITVJ?
A172 cell M2XjVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1ziWGlvcGmkaYTpc44hd2ZiaIXtZY4hSTF5MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlkyPSEQvF2= MnG5V2FPT0WU
human BCPAP cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYm0fWJvUW6qaXLpeIlwdiCxZjDoeY1idiCEQ2DBVEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjl6N{mg{txO NH\XV|hUSU6JRWK=
human COLO-792 cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFLXOmNKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tO|kzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{OUm3NkDPxE1? NH\OVoVUSU6JRWK=
human DU-145 cell NE\SSW1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2Lwb2lvcGmkaYTpc44hd2ZiaIXtZY4hTFVvMUS1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{OTh6OTFOwG0> MUTTRW5ITVJ?
NCI-H2122 cell M2P3fmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1Xn[2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNVIzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|MkK4OUDPxE1? NGr0Wo5USU6JRWK=
human SK-UT-1 cell NXP1VXBRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH;ncXdKdmirYnn0bY9vKG:oIHj1cYFvKFONLWXUMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN{OUWyJO69VQ>? NFjsPZdUSU6JRWK=
LXF-289 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoXwTY5pcWKrdHnvckBw\iCqdX3hckBNYEZvMki5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{Ojl4NTFOwG0> NEW5NG9USU6JRWK=
human NCI-H1792 cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYjsUpVNUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE4QTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkOzNFk3KM7:TR?= MVzTRW5ITVJ?
MCF7 cell M4TlPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHrpc5NKdmirYnn0bY9vKG:oIHj1cYFvKE2FRkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM{Ojd2IN88US=> NHP5dZRUSU6JRWK=
HCT-15 cell NWi5b3lOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NI[5V3dKdmirYnn0bY9vKG:oIHj1cYFvKEiFVD2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzN2M{Kg{txO MWXTRW5ITVJ?
human NCI-H358 cell NYHHZ5hYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYnCbldvUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFM2QCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{O1OVEh|ryP M2HYNHNCVkeHUh?=
human HLE cell NUDGT3ZiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1zHTWlvcGmkaYTpc44hd2ZiaIXtZY4hUEyHIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zN|c2OiEQvF2= MYXTRW5ITVJ?
human SW1088 cell NYTicIVsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4XSSWlvcGmkaYTpc44hd2ZiaIXtZY4hW1dzMEi4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{Ozd7NzFOwG0> M{[1bnNCVkeHUh?=
human K5 cell NIfZZ41Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3r6b2lvcGmkaYTpc44hd2ZiaIXtZY4hUzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkO2NVQ6KM7:TR?= MULTRW5ITVJ?
human SR cell NI\vSnhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4j2d2lvcGmkaYTpc44hd2ZiaIXtZY4hW1JiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkO2OVcyKM7:TR?= MX;TRW5ITVJ?
human Calu-3 cell M3Xl[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Moq2TY5pcWKrdHnvckBw\iCqdX3hckBE[Wy3LUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM3QDJ3IN88US=> MV\TRW5ITVJ?
human SK-MEL-30 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH7jcW1KdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0{OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{m5NVMh|ryP NWjjR4NCW0GQR1XS
human SW780 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFjGb|JKdmirYnn0bY9vKG:oIHj1cYFvKFOZN{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OTF2MjFOwG0> NY\ufYtbW0GQR1XS
NCI-H1563 cell NV\nd5A2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWL4Wox1UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE2PjNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkSxOFg1KM7:TR?= MWHTRW5ITVJ?
human MKN45 cell MorIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnTxTY5pcWKrdHnvckBw\iCqdX3hckBOU052NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFE6OzFizszN NFjoSIJUSU6JRWK=
MDA-MB-157 cell MkLkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MojOTY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtNVU4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52MkCxOUDPxE1? MYXTRW5ITVJ?
human NCI-H522 cell NHXiZ3hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIDL[JpKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IOVIzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52MkOg{txO NUTKWZI6W0GQR1XS
human A2780 cell M1LyfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1nyUGlvcGmkaYTpc44hd2ZiaIXtZY4hSTJ5OECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ4PTB|IN88US=> MXTTRW5ITVJ?
human A498 cell M2jHb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXfWcJp[UW6qaXLpeIlwdiCxZjDoeY1idiCDNEm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41PzZ7MzFOwG0> NWLpbG1bW0GQR1XS
human BxPC-3 cell NFPUe3JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUDJcohq[mm2aX;uJI9nKGi3bXHuJGJ5WENvMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFk{PjZizszN MX;TRW5ITVJ?
human A2058 cell NVjtWY04T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUTPWlZoUW6qaXLpeIlwdiCxZjDoeY1idiCDMkC1PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTJ6NESg{txO M371fnNCVkeHUh?=
human PC-14 cell NE\nbZJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVvYS49FUW6qaXLpeIlwdiCxZjDoeY1idiCSQz2xOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTN6NUWg{txO MnnJV2FPT0WU
human KG-1 cell MnrnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2HPbGlvcGmkaYTpc44hd2ZiaIXtZY4hU0dvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOVU1OTlizszN NFjuPYNUSU6JRWK=
human A375 cell MnLoS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1;CXWlvcGmkaYTpc44hd2ZiaIXtZY4hSTN5NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOVYyODNizszN NVjYPGJ6W0GQR1XS
human SW1783 cell MnvQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIC3SIdKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUe4N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzN|NzFOwG0> M{\C[nNCVkeHUh?=
human MKN1 cell NGrHW5pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MY\Jcohq[mm2aX;uJI9nKGi3bXHuJG1MVjFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLki4OFEzKM7:TR?= Mn;CV2FPT0WU
NCI-H1650 cell M4fNUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUPpSJpbUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3PTBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLki4PVE364DCzszN M{HCcnNCVkeHUh?=
human HT-1376 cell Mn7uS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXLJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTF|N{[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlkzQTF6IN88US=> MXzTRW5ITVJ?
SW872 cell NGHKeYVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NI[zSIhKdmirYnn0bY9vKG:oIHj1cYFvKFOZOEeyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE46PDR3OTFOwG0> M3;ZeXNCVkeHUh?=
human RT-112 cell M1vMUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXTCRlByUW6qaXLpeIlwdiCxZjDoeY1idiCUVD2xNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjl5NEizJO69VQ>? MYXTRW5ITVJ?
human HT-29 cell NWXaeWRQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHn6OG1KdmirYnn0bY9vKG:oIHj1cYFvKEiWLUK5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE46Pzl7NjFOwG0> NHfwVIdUSU6JRWK=
human U-266 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXzJcohq[mm2aX;uJI9nKGi3bXHuJHUuOjZ4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD65PFMxOiEQvF2= NEH4[4VUSU6JRWK=
human HEL cell NGH0WmFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVTJcohq[mm2aX;uJI9nKGi3bXHuJGhGVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwOUi1NVch|ryP MofJV2FPT0WU
human KU812 cell NWXYXZQ2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWDJcohq[mm2aX;uJI9nKGi3bXHuJGtWQDF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6xNVE3PCEQvF2= NF\5SWpUSU6JRWK=

... 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]
+ Expand
  • 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]
+ Expand
  • Animal Models: Colo 205 colorectal tumors xenograft
  • Formulation: sterile water
  • 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)
Ethanol 20 mg/mL warmed (35.04 mM)
Water Insoluble
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

Bio Calculators

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

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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).

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

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

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04097470 Not yet recruiting Drug: Decitabine|Drug: Midostaurin AML/MDS Stichting Hemato-Oncologie voor Volwassenen Nederland|Swiss Group for Clinical Cancer Research September 16 2019 Phase 2
NCT03951961 Not yet recruiting Drug: Midostaurin Acute Myeloid Leukemia Adult Sebastian Scholl PD Dr. med.|Ludwig-Maximilians - University of Munich|University of Jena July 1 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

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PKC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID