Midostaurin (PKC412)

Name: Midostaurin (PKC412)
Brand: Selleck Chemicals
SKU: S8064
Rating: 5 (20 reviews)

For research use only.

Catalog No.S8064 Synonyms: CGP 41251

20 publications

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.

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

Br J Cancer, 2020, 10.1038/s41416-020-0731-z

PubMed: 32015510 ( click the link to review the publication )

Eur J Med Chem, 2020, 193:112232

PubMed: 32199135 ( click the link to review the publication )

Transl Oncol, 2020, 1;13(4):100766

PubMed: 32247263 ( click the link to review the publication )

Cancer Chemother Pharmacol, 2020, 10.1007/s00280-020-04114-z

PubMed: 32748108 ( click the link to review the publication )

Cancers (Basel), 2020, 12(9):E2341

PubMed: 32825035 ( click the link to review the publication )

Haematologica, 2020, haematol.2019.231944

PubMed: 32616529 ( click the link to review the publication )

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 )

Blood, 2018, 25;131(4):426-438

PubMed: 29187377 ( 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 )

Nat Commun, 2017, 1;8(1):1232

PubMed: 29089541 ( 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 )

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	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 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 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)
	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 Download Midostaurin (PKC412) SDF

Molecular Weight	570.64
Formula	C₃₅H₃₀N₄O₄
CAS No.	120685-11-2
Storage	3 years-20°C powder 2 years-80°C 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)

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Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

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

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The Serial Dilution Calculator Equation

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Computed Result

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Molecular Weight Calculator

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

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To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-09-01)

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

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PKC Signaling Pathway Map

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Midostaurin (PKC412)