Midostaurin

製品コードS8064 バッチS806404

印刷

化学情報

Chemical Structure Synonyms PKC412, CGP 41251 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C35H30N4O4
分子量 570.64 CAS No. 120685-11-2
Solubility (25°C)* 体外 DMSO 100 mg/mL (175.24 mM)
Ethanol (warmed with 50ºC water bath) 39 mg/mL (68.34 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Midostaurin 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.
in vitro Midostaurin(pkc412) is a broad spectrum protein kinase inhibitor. This compound 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. It inhibits the growth of various human and animal cell lines in vitro at similar submicromolar concentrations. This chemical 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. It is able to reverse the p-glycoprotein-mediated multidrug resistance of tumor cells in vitro. [1]
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 this compound, as well as the synergy with cytotoxic agents, including doxorubicin, cyclophosphamide, cisplatin and gemcitabine. When given orally, the maximally tolerated dose for this chemical is >300 mg/kg. [1]

プロトコル(参考用のみ)

細胞アッセイ 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.
動物実験 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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/10454207/
  • https://pubmed.ncbi.nlm.nih.gov/8822090/

カスタマーフィードバック

Data from [Data independently produced by , , Leukemia, 2018, 32(1):139-148]

Data from [Data independently produced by , , J Cell Physiol, 2018, 233(12):9437-9446]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The lncRNA ELDR suppresses tumorigenicity of AML by interfering with DNA replication and chromatin accessibility [ Blood Adv, 2025, bloodadvances.2024015427] PubMed: 40921006
Anti-Tumor Effects of Gilteritinib on FLT3 Mutations: Insights into Resistance Mechanisms in Ba/F3 Cell Models [ Onco Targets Ther, 2025, 18:489-501] PubMed: 40196870
RSK1 dependency in FLT3-ITD acute myeloid leukemia [ Blood Cancer J, 2024, 14(1):207] PubMed: 39592591
Unveiling the signaling network of FLT3-ITD AML improves drug sensitivity prediction [ Elife, 2024, 12RP90532] PubMed: 38564252
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862] PubMed: 39319271
The Immunomodulatory Effect of Different FLT3 Inhibitors on Dendritic Cells [ Cancers (Basel), 2024, 16(21)3719] PubMed: 39518156
Activation of the receptor KIT induces the secretion of exosome-like small extracellular vesicles [ J Extracell Biol, 2024, 3(1):e139] PubMed: 38938682
Targeting FLT3 with a new-generation antibody-drug conjugate in combination with kinase inhibitors for treatment of AML [ Blood, 2023, 141(9):1023-1035] PubMed: 35981498
ABCC1 and glutathione metabolism limit the efficacy of BCL-2 inhibitors in acute myeloid leukemia [ Nat Commun, 2023, 14(1):5709] PubMed: 37726279
A combinatorial therapeutic approach to enhance FLT3-ITD AML treatment [ Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286] PubMed: 37951217

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。