Midostaurin

Midostaurin is a pivotal pharmaceutical API and analytical reference standard in the treatment of hematological malignancies, functioning as a multi-targeted tyrosine kinase inhibitor with potent antiangiogenic and antineoplastic activities . As the first FLT3 inhibitor approved for AML, Midostaurin is indicated in combination with standard cytarabine and daunorubicin induction and cytarabine consolidation chemotherapy for adult patients with newly diagnosed FLT3 mutation-positive AML . Midostaurin also serves as a treatment for aggressive systemic mastocytosis (ASM), systemic mastocytosis with associated haematological neoplasms (SM-AHN), and mast cell leukaemia (MCL) . Midostaurin has a molecular weight of 570.64 g/mol and appears as a solid, with purity grades available from ≥98% to >99% . Midostaurin is supplied with detailed characterization data and serves as both the API for commercial Rydapt® production and a reference standard for analytical method development and quality control applications.

Product Parameters

Application

Midostaurin exhibits anti-proliferative properties by inhibiting protein kinase C, kinase insert domain receptor and C-kit.

Bioactivity

Midostaurin (pkc412, CGP 41251) is a multi-target kinase inhibitor that acts on PKCα/β/γ， Syk， Flk-1， Akt， PKA， c-Kit， c-Fgr， c-Src， FLT3， PDFRβ and VEGFR1/2，IC50 for 80-500 nM.

In vivo studies

In addition to directly inhibiting tumor cell proliferation (by acting on PKCs), Midostaurin (pkc412) also suppresses tumor growth by inhibiting tumor angiogenesis (by acting on VEGF receptor tyrosine kinases). Midostaurin (pkc412) acts synergistically with cytotoxic agents, including Doxorubicin, Cyclophosphamide, Cisplatin and Gemcitabine, and the resulting anti-angiogenic effect may contribute to anti-metastasis and broad anti-tumor activity. Midostaurin (pkc412) is administered orally, with a maximum tolerated dose of more than 300 mg/kg.

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Interested in Midostaurin for your AML or mastocytosis API program, impurity reference standard needs, or kinase inhibitor research? Cosperpharm is ready to support your project. Contact our team today for a quote, technical documentation, or to discuss your specific requirements—we're here to help you succeed.