Midostaurin (PKC412)

製品コード:S8064 別名:CGP 41251

For research use only.

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.

Midostaurin (PKC412)化学構造

CAS No. 120685-11-2

サイズ 価格(税別)
JPY 18800
JPY 86800

代表番号: 03-5615-9297|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(33)

製品安全説明書

PKC阻害剤の選択性比較

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生物活性

製品説明 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.
ターゲット
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)
もっとクリックする
22 nM 24 nM 30 nM 31 nM 38 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EOL-1 NHG4O21EgXSxdH;4bYNqfHliYYPzZZk> MljNO|IhcHK| MXrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDFU2wuOSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRUKGG|c3H5MEBKSzVyIE2gNE4xODN6IN88UU4> NUC4b49QRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmzOVA6OjBpPkK5N|UxQTJyPD;hQi=>
MOLM13 NHXadopEgXSxdH;4bYNqfHliYYPzZZk> M3fBSVczKGi{cx?= MYHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNU2xOOTNiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VWyCjc4PhfUwhUUN3MDC9JFAvODB2NzFOwG0v M2\6PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7M{WwPVIxLz5{OUO1NFkzODxxYU6=
MV4-11 M3XpTGN6fG:2b4jpZ4l1gSCjc4PhfS=> NEOzPHM4OiCqcoO= M{DkN2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1XPC1zMTDj[YxteyCjZoTldkA4OiCqcoOgZpkh[2WubDD0bZRmei2kbIXlJIF{e2G7LDDJR|UxKD1iMD6wNVIh|ryPLh?= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTZ3NESwPEc,OTl4NUS0NFg9N2F-
RS4-11 M3LCPGZ2dmO2aX;uJIF{e2G7 MoPtNkBpenN? MXfJcohq[mm2aX;uJI9nKE[OVEOgTXRFKG23dHHueEBifXSxcHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKFKVND2xNUBk\WyuczDh[pRmeiB{IHjyd{BjgSCnbHXjeJJw[2inbXnseY1qdmW|Y3XuZ4Uh[XO|YYmsJGlEPTBiPTCwMlAyOyEQvF2u NIHjTpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOU[1OFQxQCd-MUm2OVQ1ODh:L3G+
RS4-11 NGjtUJhHfW6ldHnvckBie3OjeR?= Mn\NNkBpenN? MmjoTY5pcWKrdHnvckBw\iCITGSzJIF2fG:yaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hWlN2LUGxJINmdGy|IHHmeIVzKDJiaILzJIJ6KGWuZXP0do9kcGWvaXz1cYlv\XOlZX7j[UBie3OjeTygTWM2OCB;IECuNFE2KM7:TT6= M4jrZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NkW0OFA5Lz5zOU[1OFQxQDxxYU6=
Sf9 MnzHSpVv[3Srb36gZZN{[Xl? MVm0JIhzew>? NUXCSXNjUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgS3NVNXSjZ3fl[EBHVFR|IHvpcoF{\SCmb33hbY4hMFl3NkegeI8hWzl7MzmgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiaX7z[YN1KFOoOTDj[YxteyC3c3nu[{BJ\XJ{IIDldJRq\GViYYOgd5Vje3S{YYTlJIFnfGW{IESgbJJ{KGK7IFvpcoF{\S2JbH:gZZN{[XluIFnDOVAhRSByLkCzO{DPxE1w NXvVTIFORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFExOjNpPkK2NFgyODJ|PD;hQi=>
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MOLM-13 NV3afJJNTnWwY4Tpc44h[XO|YYm= MojuO|IhcHK| NXnuRVZjUW6qaXLpeIlwdiCxZjDGUHQ{KEmWRDDo[ZRmem:8eXfveZMhdXW2YX70JIlvKGi3bXHuJG1QVE1vMUOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCJSUWwJF0hOC5yNUWg{txONg>? M2fGWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEixNFI{Lz5{NkC4NVAzOzxxYU6=
Sf9 MXLGeY5kfGmxbjDhd5NigQ>? NUfBTVVxQTBibXnudy=> NVzBOFBKUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBIW1RvdHHn[4VlKEG3cn;yZU1CKGurbnHz[UBld22jaX6gLHMyOjNidH:gV|QxOSliKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gbY5{\WO2IGPmPUBk\WyuczD1d4lv\yC2ZYTyZUhNWlKDU1zHLUBx\XC2aXTlJIF{KHO3YoP0doF1\SCjZoTldkA6OCCvaX7zJIJ6KEurbnHz[U1IdG9iYYPzZZktKEmFNUCgQUAxNjB6IN88UU4> MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MUCyN{c,OjZyOEGwNlM9N2F-
FDC-P1 NHnTOVVHfW6ldHnvckBie3OjeR?= M2XDXFQ5KGi{cx?= MXXJcohq[mm2aX;uJI9nKGi3bXHuJGZOWyCneIDy[ZN{\WRiaX6g[5Jwf3SqIH\hZ5RweiCmZYDlcoRmdnRibX;1d4UhTkSFLWCxJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiRl3TMY1m\GmjdHXkJINmdGxicILvcIln\XKjdHnvckBqdiCycnXz[Y5k\SCqdX3hckBEW0ZzIHHmeIVzKDR6IHjyd{BjgSC{ZYPhfpVzcW5iZInlJJJm\HWldHnvckBie3OjeTygTWM2OCB;IECuNVQzKM7:TT6= NYXIPHp[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxOVY3QDlpPkKwNVU3Pjh7PD;hQi=>
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FDC-P1 NVHaUo92TnWwY4Tpc44h[XO|YYm= M1njXFQ5KGi{cx?= MmDvTY5pcWKrdHnvckBw\iCvb4Xz[UBIVS2FU1[td5RqdXWuYYTl[EBk\WyuIIDyc4xq\mW{YYTpc44hd2ZiZ4Lve5RpKG[jY4TvdkBl\XCnbnTlcpQhdW:3c3WgSmRENVBzIHPlcIx{KGW6cILld5NqdmdiaIXtZY4hTk2VIHHmeIVzKDR6IHjyd{BjgSC{ZYPhfpVzcW5iZInlJJJm\HWldHnvckBie3OjeTygTWM2OCB;IECuNkDPxE1w NUjQOWRqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxOVY3QDlpPkKwNVU3Pjh7PD;hQi=>
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Sf9 MmPiSpVv[3Srb36gZZN{[Xl? NWfnPIlmOTJyIH3pcpM> NUKyb21LUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBIW1RvdHHn[4VlKF[HR1\SNkBscW6jc3Wg[I9u[WmwIDjWO|g6KHSxIG[xN|U3MSBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDpcpNm[3RiU3[5JINmdGy|IIXzbY5oKHCxbInHcJU1QlS7cjDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBi\nSncjCxNlAhdWmwczDifUBMcW6jc3WtS4xwKGG|c3H5MEBKSzVyIE2gNE4zPSEQvF2u MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MUCyN{c,OjZyOEGwNlM9N2F-
RS4:11 MmXpSpVv[3Srb36gZZN{[Xl? MoP6O|IhcHK| NIq0W2JKdmirYnn0bY9vKG:oIIfpcIQhfHmyZTDoc41wgnmpb4XzJGZNXDNiaX6gbJVu[W5iUmO0PlEyKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IECuOEDPxE1w NYS2eY5mRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFExOjNpPkK2NFgyODJ|PD;hQi=>
U937 NW\NeodUS3m2b4TvfIlkcXS7IHHzd4F6 MYC3NkBpenN? NGTBU5VEgXSxdH;4bYNqfHliYXfhbY5{fCCITGSzMYRm\mmlaXXueEBpfW2jbjDVPVM4KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IEGuOEDPxE1w MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MUCyN{c,OjZyOEGwNlM9N2F-
SJ-GBM2 MmKydWhVWyCjc4PhfS=> M1vjNZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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SK-N-MC NXj1fXFoeUiWUzDhd5NigQ>? MXzxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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NCI-H727 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnm0TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEeyO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOTFwMUO5NkDPxE1w NIXvdpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw3ODh3M{OvK|5USU6JRWK8M4E,
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アッセイ
Methods Test Index PMID
Western blot PKCα / PKCβ1 / PKCβ2 / PKCγ / PKCη / p-PKC / p-Bad / Bad / p-Bcl2 / Bcl-2 / p-p65 / p65 ; p-TYR / p-STAT5 / STAT5 / p-S6 / S6 / p-MAPK / MAPK / p-AKT / AKT 30584254 28881711
体内試験 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]

お薦めの試験操作(参考用のみ)

細胞試験:[2]
  • 細胞株:A549, NCI-H520
  • 濃度: ~1.0 μM
  • 反応時間:24-72 h
  • 実験の流れ: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.
動物試験:[1]
  • 動物モデル:Colo 205 colorectal tumors xenograft
  • 投薬量:50 mg/kg, 200 mg/kg, once daily
  • 投与方法:p.o.

溶解度 (25°C)

体外

体内

左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
5% DMSO+45% PEG 300+ddH2O
混合させたのち直ちに使用することを推奨します。

4mg/mL

化学情報

分子量 570.64
化学式

C35H30N4O4

CAS No. 120685-11-2
Storage 3年 -20°C
2年 -80°C in solvent
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

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

便利ツール

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03951961 Terminated Drug: Midostaurin Acute Myeloid Leukemia Adult University of Jena|Ludwig-Maximilians - University of Munich March 20 2020 Phase 2
NCT04097470 Active not recruiting Drug: Decitabine|Drug: Midostaurin AML/MDS Stichting Hemato-Oncologie voor Volwassenen Nederland|Swiss Group for Clinical Cancer Research December 5 2019 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

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