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Midostaurin is a multi-target protein kinase inhibitor being investigated for the treatment of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS). It is a semi-synthetic derivative of staurosporine, an alkaloid from the bacterium Streptomyces staurosporeus. Synonyms: PKC412; PKC-412; PKC 412; PKC412A; PKC-412A; PKC 412A; CGP41251; CGP 41251; CGP-41251; Benzoylstaurosporine; 4'-N-Benzoylstaurosporine. Grade: ≥98%. CAS No. 120685-11-2. Molecular formula: C35H30N4O4. Mole weight: 570.65.
Midostaurin
Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ , Syk , Flk-1 , Akt , PKA , c-Kit , c-Fgr , c-Src , FLT3 , PDFRβ and VEGFR1/2 with IC 50 s ranging from 22-500 nM [1] [2]. Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: PKC412; CGP 41251. CAS No. 120685-11-2. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-10230.
3-Hydroxy Midostaurin, a metabolite of midostaurin (PKC412), effectively inhibits FLT3 autophosphorylation with IC50s of about 132 nM and 9.8 μM in culture medium and plasma, respectively. It is less selective but more cytotoxic than PKC412. Synonyms: CGP52421; 7-Hydroxy-PKC412; Benzamide, N-[(6S,7R,8R,10R)-7,8,9,10,17,18-hexahydro-18-hydroxy-7-methoxy-6-methyl-16-oxo-6,10-epoxy-6H,16H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-8-yl]-N-methyl-. Grade: ≥97%. CAS No. 179237-49-1. Molecular formula: C35H30N4O5. Mole weight: 586.64.
3-Hydroxy Midostaurin
3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC 50 s 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]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: CGP52421. CAS No. 179237-49-1. Pack Sizes: 1 mg. Product ID: HY-108263.
(R)-3-Hydroxy Midostaurin
(R)-3-Hydroxy Midostaurin, a potent kinases inhibitor, is a major metabolite of midostaurin undergoing by the hepatic CYP3A4 enzyme. It has the potential for the treatment of acute myeloid leukemia (AML). Synonyms: (R)-CGP52421; Benzamide, N-((3R,9S,10R,11R,13R)-2,3,10,11,12,13-hexahydro-3-hydroxy-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1H,9H-diindolo(1,2,3-gh:3',2',1'-lm)pyrrolo(3,4-j)(1,7)benzodiazonin-11-yl)-N-methyl-; 3-Hydroxy Midostaurin Epimer 2; CGP52421 Epimer 2. Grade: ≥95%. CAS No. 155848-20-7. Molecular formula: C35H30N4O5. Mole weight: 586.64.
(S)-3-Hydroxy Midostaurin
(S)-3-Hydroxy Midostaurin, a potent kinase inhibitor with IC50s of <400 nM for 13 kinases (VEGFR-2, TRK-A, FLT3, et), is a minor metabolite of midostaurin undergoing by the hepatic CYP3A4 enzyme. It has the potential for the treatment of acute myeloid leukemia (AML). Synonyms: (S)-CGP52421; Benzamide, N-((3S,9S,10R,11R,13R)-2,3,10,11,12,13-hexahydro-3-hydroxy-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1H,9H-diindolo(1,2,3-gh:3',2',1'-lm)pyrrolo(3,4-j)(1,7)benzodiazonin-11-yl)-N-methyl-; 3-Hydroxy Midostaurin Epimer 1; CGP52421 Epimer 1. Grade: ≥95%. CAS No. 945260-14-0. Molecular formula: C35H30N4O5. Mole weight: 586.64.
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