3-Hydroxy Midostaurin (Synonyms: CGP52421) |
| カタログ番号GC39689 |
PKC412 の代謝産物である 3-ヒドロキシ ミドスタウリン (CGP 52421) は、FMS 様チロシン キナーゼ 3 (FLT3) 自己リン酸化を効果的に阻害し、培養液および血漿中の IC50 はそれぞれ約 132 nM および 9.8 μM です。 3-ヒドロキシ ミドスタウリンは、PKC412 よりも選択性は低くなりますが、細胞毒性は高くなります。
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Cas No.: 179237-49-1
Sample solution is provided at 25 µL, 10mM.
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3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412[1].
[1]. Levis M, et al. Plasma inhibitory activity (PIA): a pharmacodynamic assay reveals insights into the basis for cytotoxic response to FLT3 inhibitors. Blood. 2006 Nov 15;108(10):3477-83.
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