Midostaurin (PKC412)

Name: Midostaurin (PKC412)
Brand: Selleck Chemicals
SKU: S8064
Rating: 5 (13 reviews)

For research use only. Not for use in humans.

Catalog No.S8064 Synonyms: CGP 41251

13 publications

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.

Selleck's Midostaurin (PKC412) has been cited by 13 publications

Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-0832

PubMed: 31320594 ( click the link to review the publication )

Cancer Res, 2019, 10.1158/0008-5472

PubMed: 31270078 ( click the link to review the publication )

Cancer Lett, 2019, 445:34-44

PubMed: 30639533 ( click the link to review the publication )

Oncogenesis, 2019, 8(8):39

PubMed: 31311917 ( click the link to review the publication )

Leukemia, 2018, 32(1):139-148

PubMed: 28663576 ( click the link to review the publication )

Leukemia, 2018, 32(2):313-322

PubMed: 28895560 ( click the link to review the publication )

Cell Death Dis, 2018, 10(1):8

PubMed: 30584254 ( click the link to review the publication )

J Cell Physiol, 2018, 233(12):9437-9446

PubMed: 29968910 ( click the link to review the publication )

Oncotarget, 2018, 9(89):35962-35973

PubMed: 30542510 ( click the link to review the publication )

PLoS One, 2017, 12(8):e0183161

PubMed: 28817624 ( click the link to review the publication )

PLoS One, 2017, 12(8):e0183161

PubMed: 28817624 ( click the link to review the publication )

Sci Adv, 2015, 1(8):e1500221

PubMed: 26601252 ( click the link to review the publication )

Elife, 2014, 3

PubMed: 25531068 ( click the link to review the publication )

2 Customer Reviews

(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

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)	View More
22 nM	24 nM	30 nM	31 nM	38 nM	View More

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	Incubation Time	Activity Description	PMID
human MV4-11 cells	M1nZ[WN6fG:2b4jpZ4l1gSCjc4PhfS=>	NUjk[IEzPzJiaB?=	M4LMc2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1XPC1zMTDj[YxteyCjZoTldkA4OiCqcoOgZpkh[2WubDD0bZRmei2kbIXlJIF{e2G7LDDJR\|UxRTF{IH7N	MVKxPVY2PDRyOB?=
RS4-11 cells	NH[xfpVHfW6ldHnvckBie3OjeR?=	NVrIe2NZOiCq	NIqwU3ZKdmirYnn0bY9vKG:oIF\MWFMhUVSGIH31eIFvfCCjdYTvdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIGLTOE0yOSClZXzsd{Bi\nSncjCyJIhzeyCkeTDlcIVkfHKxY3jlcYltfW2rbnXzZ4Vv[2ViYYPzZZktKEmFNUC9NVMhdk1?	MUSxPVY2PDRyOB?=
CGTH-W-1 cell	NF7tPI5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MXfJcohq[mm2aX;uJI9nKGi3bXHuJGNIXEhvVz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFIvPjVizszN	MWTTRW5ITVJ?
SW982 cell	MnL1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NFjMe2hKdmirYnn0bY9vKG:oIHj1cYFvKFOZOUiyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFUvPThizszN	NF3SOphUSU6JRWK=
human EoL-1-cell cell	M4W5fGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MX7Jcohq[mm2aX;uJI9nKGi3bXHuJGVwVC1zLXPlcIwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Oi5yODDuUS=>	MlH2V2FPT0WU
MOLM-13 cells	MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M3rLV\|czKGh?	M4DYNmlvcGmkaYTpc44hd2ZiRlzUN{BKXERiaHX0[ZJwgnmpb4XzJI12fGGwdDDpckBpfW2jbjDNU2xONTF\|IHPlcIx{KGG\|c3Xzd4VlKGG\|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO\|IhcHK\|IHL5JG1VWyCjc4PhfUwhT0l3ME2wMlA2PSEQvF2=	NVKzN\|N5OjZyOEGwNlM>
KASUMI-1 cell	MoXLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NWq3W\|dyUW6qaXLpeIlwdiCxZjDoeY1idiCNQWPVUWkuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTBwME[wNVYh\|ryP	NIfKW2VUSU6JRWK=
NCI-H1755 cell	Ml[xS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NWW5epdwUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE4PTViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkC2Nlc{KM7:TR?=	NXrN[WcxW0GQR1XS
human MES-SA cell	MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		MVHJcohq[mm2aX;uJI9nKGi3bXHuJG1GWy2VQTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuNFc2PDRizszN	MWDTRW5ITVJ?
human HCC1395 cell	MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		Mk\WTY5pcWKrdHnvckBw\iCqdX3hckBJS0NzM{m1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xQDR{ODFOwG0>	NELsZ2hUSU6JRWK=
human D-336MG cell	NXfWUndJT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MUnJcohq[mm2aX;uJI9nKGi3bXHuJGQuOzN4TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlA5PzV2IN88US=>	MoPYV2FPT0WU
CHP-212 cell	Ml;5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NWn4eYdLUW6qaXLpeIlwdiCxZjDoeY1idiCFSGCtNlEzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5yOEe3N{DPxE1?	NHr5SWdUSU6JRWK=
human KM12 cell	NUDwbWo1T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MYLJcohq[mm2aX;uJI9nKGi3bXHuJGtOOTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkC5Nlc2KM7:TR?=	NVrSWVJNW0GQR1XS
A204 cell	Mn7PS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		M1;U[GlvcGmkaYTpc44hd2ZiaIXtZY4hSTJyNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuNVAxPTJizszN	M{Dv[nNCVkeHUh?=
CAL-51 cell	MnTJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MXzJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC13MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuNVA4ODlizszN	NWPTN5I1W0GQR1XS
human A431 cell	NIDNXJZIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NEXSeZNKdmirYnn0bY9vKG:oIHj1cYFvKEF2M{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEyOjF4IN88US=>	M3PhTnNCVkeHUh?=
NCI-H650 cell	NGTpe5JIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M2Kyc2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi2OVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjFzN{C4JO69VQ>?	MlLTV2FPT0WU
A427 cell	M1u2SGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MofSTY5pcWKrdHnvckBw\iCqdX3hckBCPDJ5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD6xNVkyQCEQvF2=	MYjTRW5ITVJ?
human 769-P cell	M{\hdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		M1XlOmlvcGmkaYTpc44hd2ZiaIXtZY4hPzZ7LWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEzODh{IN88US=>	NEHzSmlUSU6JRWK=
SW1710 cell	NXn2[ZBZT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NULtVY9PUW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF\|M{G2JO69VQ>?	M3PmSXNCVkeHUh?=
human H4 cell	MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		MXrJcohq[mm2aX;uJI9nKGi3bXHuJGg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zM{m2N{DPxE1?	Ml;ZV2FPT0WU
HT-1080 cell	M3PoOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MX;Jcohq[mm2aX;uJI9nKGi3bXHuJGhVNTFyOECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE2QTh{IN88US=>	NWr3O4xEW0GQR1XS
human PANC-03-27 cell	NVv1TFJmT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MV\Jcohq[mm2aX;uJI9nKGi3bXHuJHBCVkNvMEOtNlch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF4MEKg{txO	MlzuV2FPT0WU
A375 cells	M2rIZ2N6fG:2b4jpZ4l1gSCjc4PhfS=>	MorpO\|IhcA>?	NH;1TGhVd3irY3n0fUBi\2GrboP0JIh2dWGwIFGzO\|Uh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IHPlcIwhfGm2ZYKtZox2\SCjc4PhfUwhUUN3ME2wMlE5KM7:TR?=	NYPPSYZrOTl4NUS0NFg>
human HOP-62 cell	M{\HSmZ2dmO2aX;uJIF{e2G7		M17DNmlvcGmkaYTpc44hd2ZiaIXtZY4hUE:SLU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yQDB5MzFOwG0>	M3\jN3NCVkeHUh?=
human U031 cell	MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		NGHvSYlKdmirYnn0bY9vKG:oIHj1cYFvKFVyM{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE6Pjl6IN88US=>	MlnHV2FPT0WU
mouse BAF3 cells	MYnQdo9tcW[ncnH0bY9vKGG\|c3H5		NFLG[IVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBSlMh[2WubIOgeJJidnOob4Lt[YQhf2m2aDDaUmYyQThvRlfGVlEh[2:wc4TyeYN1NCCLQ{WwQVAvOiEQvF2=	Mnr6NlE6OzZ3NEK=
human G-402 cell	NEHkWVVIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGcuPDB{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD6yNFI2OyEQvF2=	MUjTRW5ITVJ?
human G-361 cell	NHTx[oNIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M3rwTWlvcGmkaYTpc44hd2ZiaIXtZY4hTy1\|NkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIxQDV\|IN88US=>	NGHmSXRUSU6JRWK=
NCI-H810 cell	NIP4UZNIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NFna[ZdKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IPFExKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{MUCyO{DPxE1?	MXXTRW5ITVJ?
NCI-H2030 cell	NIPOSGRIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NH3y[5pKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlA{OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTBwMkOwNFYh\|ryP	Mn3zV2FPT0WU
human HCT-116 cell	M33DXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		M1HHN2lvcGmkaYTpc44hd2ZiaIXtZY4hUEOWLUGxOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjN3Nkig{txO	MnfIV2FPT0WU
human SNU-423 cell	MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		NWHZeIhQUW6qaXLpeIlwdiCxZjDoeY1idiCVTmWtOFI{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{M{[1O{DPxE1?	MXrTRW5ITVJ?
human SCC-4 cell	M2n4T2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MUfJcohq[mm2aX;uJI9nKGi3bXHuJHNESy12IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD6yN\|k3PyEQvF2=	M4LFW3NCVkeHUh?=
human SW48 cell	NYDQdJVOT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		Moe3TY5pcWKrdHnvckBw\iCqdX3hckBUXzR6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD6yOlY5KM7:TR?=	MlW0V2FPT0WU
human SF295 cell	NWLzU41RT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NGXoZ5pKdmirYnn0bY9vKG:oIHj1cYFvKFOIMkm1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPzJ3NzFOwG0>	M4ruR3NCVkeHUh?=
MDA-MB-231 cell	MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		M{mwVWlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVI{OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTBwMkixNFEh\|ryP	NHzvb2NUSU6JRWK=
A172 cell	M2T4dmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MY\Jcohq[mm2aX;uJI9nKGi3bXHuJGEyPzJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkK5NVUh\|ryP	MYPTRW5ITVJ?
human BCPAP cell	MoTBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MnLrTY5pcWKrdHnvckBw\iCqdX3hckBDS1CDUDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuNlk5PzlizszN	MY\TRW5ITVJ?
human COLO-792 cell	NWjUTWtxT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MW\Jcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vN{myJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zQTl5MjFOwG0>	NWfpZ5hJW0GQR1XS
human DU-145 cell	NUnUNGg{T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NIf1fYpKdmirYnn0bY9vKG:oIHj1cYFvKESXLUG0OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzF6OEmg{txO	Mkj2V2FPT0WU
NCI-H2122 cell	NHPRUXlIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MlnzTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKxNlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN{Mki1JO69VQ>?	NULj[WViW0GQR1XS
human SK-UT-1 cell	NVfUTXlCT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NEO4UlBKdmirYnn0bY9vKG:oIHj1cYFvKFONLWXUMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN{OUWyJO69VQ>?	NH3IZY9USU6JRWK=
LXF-289 cell	MlvYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MVLJcohq[mm2aX;uJI9nKGi3bXHuJGxZTi1{OEmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzQTZ3IN88US=>	Ml3aV2FPT0WU
human NCI-H1792 cell	Ml7PS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NF;HRWZKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVc6OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTBwM{OwPVYh\|ryP	MXLTRW5ITVJ?
MCF7 cell	MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		NYG2XYtVUW6qaXLpeIlwdiCxZjDoeY1idiCPQ1[3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{OzJ5NDFOwG0>	MnvaV2FPT0WU
HCT-15 cell	M2LJVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NHnLZlRKdmirYnn0bY9vKG:oIHj1cYFvKEiFVD2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzN2M{Kg{txO	MWjTRW5ITVJ?
human NCI-H358 cell	MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		M4jR[WlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVizOVgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN\|NUWxJO69VQ>?	MlvaV2FPT0WU
human HLE cell	NYDvVVhsT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NYrWSopNUW6qaXLpeIlwdiCxZjDoeY1idiCKTFWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM{PzV{IN88US=>	M2KxeXNCVkeHUh?=
human SW1088 cell	MnzoS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NGH4dWxKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUC4PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzN5OUeg{txO	MYPTRW5ITVJ?
human K5 cell	NVfU[ZF5T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		M3nq[2lvcGmkaYTpc44hd2ZiaIXtZY4hUzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkO2NVQ6KM7:TR?=	NHOwR4lUSU6JRWK=
human SR cell	MmnIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MXjJcohq[mm2aX;uJI9nKGi3bXHuJHNTKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5\|NkW3NUDPxE1?	MXnTRW5ITVJ?
human Calu-3 cell	MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		MXfJcohq[mm2aX;uJI9nKGi3bXHuJGNidHVvMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuN\|Y5OjVizszN	Mk\TV2FPT0WU
human SK-MEL-30 cell	NFfvcnhIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NIfPNJhKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0{OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTBwM{m5NVMh\|ryP	M372U3NCVkeHUh?=
human SW780 cell	MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		NUKwcpJYUW6qaXLpeIlwdiCxZjDoeY1idiCVV{e4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDFzNEKg{txO	NYrwflEyW0GQR1XS
NCI-H1563 cell	NFr2ZZhIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MV\Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUW2N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDF2OESg{txO	NFrBTFBUSU6JRWK=
human MKN45 cell	M1;Xdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MVfJcohq[mm2aX;uJI9nKGi3bXHuJG1MVjR3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD60NVk{OSEQvF2=	NH;0T3lUSU6JRWK=
MDA-MB-157 cell	MmD4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NGD2ZZRKdmirYnn0bY9vKG:oIHj1cYFvKE2GQT3NRk0yPTdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkSyNFE2KM7:TR?=	M1nRW3NCVkeHUh?=
human NCI-H522 cell	MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		NGnPcJRKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IOVIzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52MkOg{txO	NHvFeFdUSU6JRWK=
human A2780 cell	NW\GZ491T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		Mkn3TY5pcWKrdHnvckBw\iCqdX3hckBCOjd6MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuOFc2ODNizszN	MnTTV2FPT0WU
human A498 cell	NWL3N2FQT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NXvHUIx{UW6qaXLpeIlwdiCxZjDoeY1idiCDNEm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41PzZ7MzFOwG0>	MXjTRW5ITVJ?
human BxPC-3 cell	MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		MYrJcohq[mm2aX;uJI9nKGi3bXHuJGJ5WENvMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuOFk{PjZizszN	NEDDR4JUSU6JRWK=
human A2058 cell	NHezW3dIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M3fZfGlvcGmkaYTpc44hd2ZiaIXtZY4hSTJyNUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlUzQDR2IN88US=>	Mnj4V2FPT0WU
human PC-14 cell	NVT1cXZ2T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NFr1PFVKdmirYnn0bY9vKG:oIHj1cYFvKFCFLUG0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE42Ozh3NTFOwG0>	NHnzUHJUSU6JRWK=
human KG-1 cell	M3\WbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MWTJcohq[mm2aX;uJI9nKGi3bXHuJGtINTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkW1OFE6KM7:TR?=	NVPyVHNOW0GQR1XS
human A375 cell	MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		NGTBWodKdmirYnn0bY9vKG:oIHj1cYFvKEF\|N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU3OTB\|IN88US=>	MXLTRW5ITVJ?
human SW1783 cell	M4TLWWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		M4[5cWlvcGmkaYTpc44hd2ZiaIXtZY4hW1dzN{izJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44OzN5IN88US=>	NYrBZ4ZFW0GQR1XS
human MKN1 cell	MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		NGf4UpJKdmirYnn0bY9vKG:oIHj1cYFvKE2NTkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlg5PDF{IN88US=>	NXPZV2VmW0GQR1XS
NCI-H1650 cell	M3ntVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		M{\U[WlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOlUxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC56OEmxOwOBiM7:TR?=	MoX1V2FPT0WU
human HT-1376 cell	MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		MnfvTY5pcWKrdHnvckBw\iCqdX3hckBJXC1zM{e2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE46OjlzODFOwG0>	MV7TRW5ITVJ?
SW872 cell	MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		Mm\TTY5pcWKrdHnvckBw\iCqdX3hckBUXzh5MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuPVQ1PTlizszN	NYG4PXJ5W0GQR1XS
human RT-112 cell	NUDjbWJXT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MXTJcohq[mm2aX;uJI9nKGi3bXHuJHJVNTFzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuPVc1QDNizszN	MX\TRW5ITVJ?
human HT-29 cell	Mn;HS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MVfJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTJ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD65O\|k6PiEQvF2=	MVTTRW5ITVJ?
human U-266 cell	MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		MYTJcohq[mm2aX;uJI9nKGi3bXHuJHUuOjZ4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD65PFMxOiEQvF2=	M1PUZXNCVkeHUh?=
human HEL cell	Mn;uS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		M4X1cGlvcGmkaYTpc44hd2ZiaIXtZY4hUEWOIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD65PFUyPyEQvF2=	MmfXV2FPT0WU
human KU812 cell	MmH6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NUnWNm9yUW6qaXLpeIlwdiCxZjDoeY1idiCNVUixNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOTFzNkSg{txO	NXHVe4JjW0GQR1XS

... 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 Oncotarget 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 Cell Death Dis 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)

References

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 Download Midostaurin (PKC412) SDF

Molecular Weight	570.64
Formula	C₃₅H₃₀N₄O₄
CAS No.	120685-11-2
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	CGP 41251

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-10-14)

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

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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.

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PKC Signaling Pathway Map

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Midostaurin (PKC412)