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 12 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 NUjRVGlQS3m2b4TvfIlkcXS7IHHzd4F6 M3LN[FczKGh? MXrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNWlQuOTFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JINmdGxidHn0[ZIu[my3ZTDhd5NigSxiSVO1NF0yOiCwTR?= MV[xPVY2PDRyOB?=
RS4-11 cells NHTWSmZHfW6ldHnvckBie3OjeR?= Ml\qNkBp MlO2TY5pcWKrdHnvckBw\iCITGSzJGlVTCCvdYThcpQh[XW2b4Doc5NxcG:{eXzheIlwdiCrbjDoeY1idiCUU{StNVEh[2WubIOgZYZ1\XJiMjDodpMh[nliZXzlZ5Rzd2OqZX3pcJVucW6nc3PlcoNmKGG|c3H5MEBKSzVyPUGzJI5O MWWxPVY2PDRyOB?=
CGTH-W-1 cell MnnWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3LYXWlvcGmkaYTpc44hd2ZiaIXtZY4hS0eWSD3XMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Oi54NTFOwG0> MULTRW5ITVJ?
SW982 cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXTkfFMxUW6qaXLpeIlwdiCxZjDoeY1idiCVV{m4NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ2NjV6IN88US=> MmnLV2FPT0WU
human EoL-1-cell cell M4n6WWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYjJcohq[mm2aX;uJI9nKGi3bXHuJGVwVC1zLXPlcIwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Oi5yODDuUS=> M1TNOnNCVkeHUh?=
MOLM-13 cells MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmXHO|IhcA>? Ml3STY5pcWKrdHnvckBw\iCITGSzJGlVTCCqZYTldo97gWexdYOgcZV1[W62IHnuJIh2dWGwIF3PUG0uOTNiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgUXRUKGG|c3H5MEBIUTVyPUCuNFU2KM7:TR?= MlrSNlYxQDFyMkO=
KASUMI-1 cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWLtWGlVUW6qaXLpeIlwdiCxZjDoeY1idiCNQWPVUWkuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwME[wNVYh|ryP MW\TRW5ITVJ?
NCI-H1755 cell M2j3SWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{G5cGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixO|U2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5yNkK3N{DPxE1? M3vuWXNCVkeHUh?=
human MES-SA cell NXnQ[|hWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFT5OVBKdmirYnn0bY9vKG:oIHj1cYFvKE2HUz3TRUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODd3NESg{txO NXjRZpB1W0GQR1XS
human HCC1395 cell NU\sXoVzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYrN[mNCUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OxN|k2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5yOESyPEDPxE1? NYnHPI1rW0GQR1XS
human D-336MG cell MkfxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVXJcohq[mm2aX;uJI9nKGi3bXHuJGQuOzN4TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlA5PzV2IN88US=> NFzwT5JUSU6JRWK=
CHP-212 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml\5TY5pcWKrdHnvckBw\iCqdX3hckBEUFBvMkGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xQDd5MzFOwG0> NIDzTplUSU6JRWK=
human KM12 cell NGDjZXNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4PiR2lvcGmkaYTpc44hd2ZiaIXtZY4hU01zMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFkzPzVizszN NI\Zc|dUSU6JRWK=
A204 cell M{jLRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVLnRZdoUW6qaXLpeIlwdiCxZjDoeY1idiCDMkC0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yODB3MjFOwG0> MW\TRW5ITVJ?
CAL-51 cell NXLzVVJKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2nOS2lvcGmkaYTpc44hd2ZiaIXtZY4hS0GOLUWxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yODdyOTFOwG0> Mm\ZV2FPT0WU
human A431 cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEj2fG5KdmirYnn0bY9vKG:oIHj1cYFvKEF2M{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEyOjF4IN88US=> NWDY[XhKW0GQR1XS
NCI-H650 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUHoW4dEUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFY2OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUG3NFgh|ryP NVHoTY9TW0GQR1XS
A427 cell M1Ltcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3[zUGlvcGmkaYTpc44hd2ZiaIXtZY4hSTR{NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVE6OThizszN NH3lU4xUSU6JRWK=
human 769-P cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1TR[mlvcGmkaYTpc44hd2ZiaIXtZY4hPzZ7LWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEzODh{IN88US=> MomwV2FPT0WU
SW1710 cell M2PKc2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUTJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTdzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVM{OTZizszN NELz[VVUSU6JRWK=
human H4 cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUfqS2s1UW6qaXLpeIlwdiCxZjDoeY1idiCKNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVM6PjNizszN NIrR[otUSU6JRWK=
HT-1080 cell M3X5UGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mmr2TY5pcWKrdHnvckBw\iCqdX3hckBJXC1zMEiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yPTl6MjFOwG0> MUnTRW5ITVJ?
human PANC-03-27 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYTJcohq[mm2aX;uJI9nKGi3bXHuJHBCVkNvMEOtNlch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF4MEKg{txO MmLrV2FPT0WU
A375 cells MXXDfZRwfG:6aXPpeJkh[XO|YYm= NUXN[2tbPzJiaB?= MXvUc5hq[2m2eTDh[4FqdnO2IHj1cYFvKEF|N{WgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KGOnbHygeIl1\XJvYnz1[UBie3OjeTygTWM2OD1yLkG4JO69VQ>? MWmxPVY2PDRyOB?=
human HOP-62 cell MnTVSpVv[3Srb36gZZN{[Xl? Ml;2TY5pcWKrdHnvckBw\iCqdX3hckBJV1BvNkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE5ODd|IN88US=> M3nafXNCVkeHUh?=
human U031 cell M4O0Tmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYnJcohq[mm2aX;uJI9nKGi3bXHuJHUxOzFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG5Olk5KM7:TR?= MUTTRW5ITVJ?
mouse BAF3 cells Mlq3VJJwdGmoZYLheIlwdiCjc4PhfS=> NWKzdYhHSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDCRWY{KGOnbHzzJJRz[W6|Zn;ycYVlKHerdHigXm5HOTl6LV\HSnIyKGOxboP0dpVkfCxiSVO1NF0xNjJizszN MXmyNVk{PjV2Mh?=
human G-402 cell NGjIVotIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIHORpVKdmirYnn0bY9vKG:oIHj1cYFvKEdvNECyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zODJ3MzFOwG0> NWHZ[GpEW0GQR1XS
human G-361 cell M4DldWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV3qSoJ1UW6qaXLpeIlwdiCxZjDoeY1idiCJLUO2NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjB6NUOg{txO M2OxcXNCVkeHUh?=
NCI-H810 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXXEcXByUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFgyOCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMkGwNlch|ryP Ml;WV2FPT0WU
NCI-H2030 cell M2XNN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFvZN2VKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlA{OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMkOwNFYh|ryP M1SweHNCVkeHUh?=
human HCT-116 cell MnHIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MY\Jcohq[mm2aX;uJI9nKGi3bXHuJGhEXC1zMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI{PTZ6IN88US=> MnPyV2FPT0WU
human SNU-423 cell M1;PPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmWyTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zOzZ3NzFOwG0> MWrTRW5ITVJ?
human SCC-4 cell MnzlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYfS[olXUW6qaXLpeIlwdiCxZjDoeY1idiCVQ1OtOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjN7Nkeg{txO MV;TRW5ITVJ?
human SW48 cell NEniW3NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NF;tNWZKdmirYnn0bY9vKG:oIHj1cYFvKFOZNEigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI3PjhizszN NHjVbWVUSU6JRWK=
human SF295 cell NELDSVJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1ryfmlvcGmkaYTpc44hd2ZiaIXtZY4hW0Z{OUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI4OjV5IN88US=> MY\TRW5ITVJ?
MDA-MB-231 cell NGjDU4lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUnpU3Z7UW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuOjNzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yPFExOSEQvF2= M1PLZnNCVkeHUh?=
A172 cell NHfGNIJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUWwcI5mUW6qaXLpeIlwdiCxZjDoeY1idiCDMUeyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zQTF3IN88US=> M1XBNXNCVkeHUh?=
human BCPAP cell MmfBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXHJcohq[mm2aX;uJI9nKGi3bXHuJGJEWEGSIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yPVg4QSEQvF2= NISxc2RUSU6JRWK=
human COLO-792 cell M3zhR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M37YVWlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz23PVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ7OUeyJO69VQ>? M{fmWHNCVkeHUh?=
human DU-145 cell M4j6OGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2O1OWlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvMUS1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{OTh6OTFOwG0> Mn;uV2FPT0WU
NCI-H2122 cell NVP5N|F2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWHJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkGyNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzJ{OEWg{txO NX22dmRbW0GQR1XS
human SK-UT-1 cell Ml\ES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NU\3PZE4UW6qaXLpeIlwdiCxZjDoeY1idiCVSz3VWE0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|Mkm1NkDPxE1? MUHTRW5ITVJ?
LXF-289 cell M2Dre2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH\hV2tKdmirYnn0bY9vKG:oIHj1cYFvKEy[Rj2yPFkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN{OU[1JO69VQ>? M3vhZnNCVkeHUh?=
human NCI-H1792 cell M1PkNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{S4UWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixO|kzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|M{C5OkDPxE1? MmexV2FPT0WU
MCF7 cell M123dWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWrDSIxFUW6qaXLpeIlwdiCxZjDoeY1idiCPQ1[3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{OzJ5NDFOwG0> MkXrV2FPT0WU
HCT-15 cell NGfn[oZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3zwfGlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWLUG1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{OzR|MjFOwG0> MlHvV2FPT0WU
human NCI-H358 cell NEnvSmZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYG3d4x2UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFM2QCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{O1OVEh|ryP NIHKTotUSU6JRWK=
human HLE cell NGi0VHZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYXJcohq[mm2aX;uJI9nKGi3bXHuJGhNTSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{O3OVIh|ryP MWLTRW5ITVJ?
human SW1088 cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFzLepdKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUC4PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzN5OUeg{txO M2m5dnNCVkeHUh?=
human K5 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoLNTY5pcWKrdHnvckBw\iCqdX3hckBMPSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{[xOFkh|ryP NF;FUmJUSU6JRWK=
human SR cell NIDhVIVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWjJcohq[mm2aX;uJI9nKGi3bXHuJHNTKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|NkW3NUDPxE1? MmmyV2FPT0WU
human Calu-3 cell MojOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX;SV5cyUW6qaXLpeIlwdiCxZjDoeY1idiCFYXz1MVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN4OEK1JO69VQ>? NVvGcZZLW0GQR1XS
human SK-MEL-30 cell NV\rUVdvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3m3SWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVMxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|OUmxN{DPxE1? M1f0U3NCVkeHUh?=
human SW780 cell MmLiS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4PITGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d5OECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQyOTR{IN88US=> NGTYW|BUSU6JRWK=
NCI-H1563 cell M{\adWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYHvXYs5UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE2PjNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkSxOFg1KM7:TR?= M4K3dXNCVkeHUh?=
human MKN45 cell NGfiPZBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkHZTY5pcWKrdHnvckBw\iCqdX3hckBOU052NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFE6OzFizszN MV7TRW5ITVJ?
MDA-MB-157 cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVnJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2xOVch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjR{MEG1JO69VQ>? NWLyVYJ6W0GQR1XS
human NCI-H522 cell NV7BSoVsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF\RZ3VKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IOVIzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52MkOg{txO M3fZTHNCVkeHUh?=
human A2780 cell NF60TVhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXTJcohq[mm2aX;uJI9nKGi3bXHuJGEzPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60O|UxOyEQvF2= M2DvOHNCVkeHUh?=
human A498 cell NYDEVGRoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3XQbWlvcGmkaYTpc44hd2ZiaIXtZY4hSTR7ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFc3QTNizszN NV;DepNXW0GQR1XS
human BxPC-3 cell NVOzO3VbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkS0TY5pcWKrdHnvckBw\iCqdX3hckBDgFCFLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ6OzZ4IN88US=> MmXYV2FPT0WU
human A2058 cell NF\BZmtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUTVd2pbUW6qaXLpeIlwdiCxZjDoeY1idiCDMkC1PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTJ6NESg{txO MkLkV2FPT0WU
human PC-14 cell M2\MNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3H1d2lvcGmkaYTpc44hd2ZiaIXtZY4hWENvMUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU{QDV3IN88US=> NWrYXHRyW0GQR1XS
human KG-1 cell MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4XlTGlvcGmkaYTpc44hd2ZiaIXtZY4hU0dvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOVU1OTlizszN MnXMV2FPT0WU
human A375 cell M3;aW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUnJcohq[mm2aX;uJI9nKGi3bXHuJGE{PzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkW2NVA{KM7:TR?= Ml;yV2FPT0WU
human SW1783 cell NYHRRWRXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH74eY5KdmirYnn0bY9vKG:oIHj1cYFvKFOZMUe4N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzN|NzFOwG0> NEi1bmdUSU6JRWK=
human MKN1 cell NGPufpRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mny1TY5pcWKrdHnvckBw\iCqdX3hckBOU05zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD64PFQyOiEQvF2= MXLTRW5ITVJ?
NCI-H1650 cell NGrYfpRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1;EWGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOlUxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC56OEmxOwOBiM7:TR?= MU\TRW5ITVJ?
human HT-1376 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIPqfmRKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUGzO|Yh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjl{OUG4JO69VQ>? NWrkOGhUW0GQR1XS
SW872 cell NVntU21PT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFfTWodKdmirYnn0bY9vKG:oIHj1cYFvKFOZOEeyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE46PDR3OTFOwG0> MWXTRW5ITVJ?
human RT-112 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGHzSYNKdmirYnn0bY9vKG:oIHj1cYFvKFKWLUGxNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvQTd2OEOg{txO MkXOV2FPT0WU
human HT-29 cell NX3nTZk3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIn3TXFKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUK5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE46Pzl7NjFOwG0> MUDTRW5ITVJ?
human U-266 cell NEL0[pBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXziZoR3UW6qaXLpeIlwdiCxZjDoeY1idiCXLUK2OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvQTh|MEKg{txO NFXNV5lUSU6JRWK=
human HEL cell MorxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mnr3TY5pcWKrdHnvckBw\iCqdX3hckBJTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkm4OVE4KM7:TR?= NG\sNmZUSU6JRWK=
human KU812 cell NVPrXGIzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUS4Snl1UW6qaXLpeIlwdiCxZjDoeY1idiCNVUixNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOTFzNkSg{txO NHTTZm5USU6JRWK=

... 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
  • 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

Molarity Calculator

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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