Midostaurin

Midostaurin

Catalog Number:
M001341563TOK
Mfr. No.:
TOK-M123
Price:
$285
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      • Overview
        • Midostaurin is an organic protein kinase inhibitor for tyrosine kinase, protein kinase C, and VEGF. It is an organic heterooctacyclic compound that is the N-benzoyl derivative of stauroporine, an alkaloid from Streptomyces staurosporeus. It has been studied for its potential use for acute myeloid leukemia, myelodysplastic syndrome, and systemic mastocytosis. Midostaurin is an inhibitor of FLT3 activation loop mutations. It can be used in cancer research and has anti-tumor properties. The compound is used in COVID-19 research in repurposing studies to target the SARS-CoV-2 Main protease. Midostaurin is soluble in DMSO.

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          Background

          Midostaurin is a small molecule that inhibits multiple receptor tyrosine kinases. Midostaurin and its major active metabolites inhibit the activity of protein kinase C alpha (PKCalpha), VEGFR2, KIT, PDGFR and WT and/or mutant TLT3.

      • Properties
        • CAS Number
          120685-11-2
          Molecular Formula
          C35H30N4O4
          Molecular Weight
          570.6
          Other Properties
          Source: Synthetic
          Purity Level: 98-102% (on anhydrous and solvent-free basis)
          Storage
          <30°C

          * For research use only

      • Applications
        • Application Description
          Spectrum: Midostaurin is active against fungi and protozoa. It has no antibacterial activity.

          Cancer Applications: Midostatin is an antineoplastic agent and has antiproliferative activity toward multiple cancer cell ines.
          Midostatin blocks the transport of ATP-binding cassette (ABC) protein ABCB1 and re-sensitizes ABCB1-overexpressing multidrug-resistant cancer cells to conventional chemotherapeutic compounds. Midostaurin potentiates drug-induced apoptosis in ABCB1-overexpressing cancer cells and inhibits the ATPase activity of ABCB1. This means that multidrug-resistant tumors may benefit from Midostaurin coupled with standard chemotherapeutic agents (Hsiao et al, 2019).
          Midostatin can inhibit growth; induce megakaryocytic differentiation; and to a lesser extent, cause apoptosis in human erythroleukemia (HEL) cells (Huang Y et al, 2009)

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