(S)-3-Hydroxy Midostaurin
Based on 1 Customer Validation
(S)-3-Hydroxy Midostaurin ((S)-CGP52421) is a potent kinases inhibitor with IC50 values of <400 nM for 13 kinases (VEGFR-2, TRK-A, FLT3, et). (S)-3-Hydroxy Midostaurin is a minor metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (S)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML).
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- Reinheit: 96.07%
- CAS. Nr.: 945260-14-0
- Formel: C35H30N4O5
- Molecular Weight:586.64
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
530 nM
Compound: CGP-52421
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Toxicity against human A375 cells after 72 hrs by cell titer-blue assay
Toxicity against human A375 cells after 72 hrs by cell titer-blue assay
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[PMID: 19654408] |
| MV4-11 | IC50 |
64 nM
Compound: CGP-52421
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Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay
Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay
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[PMID: 19654408] |
| RS4-11 | IC50 |
160 nM
Compound: CGP-52421
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Inhibition of FLT3 ITD mutant autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
Inhibition of FLT3 ITD mutant autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
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[PMID: 19654408] |
| RS4-11 | IC50 |
350 nM
Compound: CGP-52421
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Inhibition of FLT3 autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
Inhibition of FLT3 autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
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[PMID: 19654408] |
(S)-3-Hydroxy Midostaurin ((S)-CGP52421; compound 4) has IC50 values in the range of 200-400 nM against the ITD and D835Y mutants and low micromolar activity against the wild-type enzyme[1].
The epimeric mixture of metabolites ((R)-3-Hydroxy Midostaurin + (S)-3-Hydroxy Midostaurin) substantially inhibits the proliferation of only the Tel-PDGFRβ (GI50=63 nM), KIT D816V (GI50=320 nM), and FLT3-ITD (GI50=650 nM) BaF3 cell lines, while the wild-type cells are relatively insensitive[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 945260-14-0
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Appearance Solid
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Molecular Weight 586.64
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Formel C35H30N4O5
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Color White to off-white
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SMILES
O[C@@H]1NC(C2=C1C(C3=C4C=CC=C3)=C5N4[C@]6(C)[C@@H]([C@@H](C[C@](O6)([H])N7C5=C2C8=C7C=CC=C8)N(C(C9=CC=CC=C9)=O)C)OC)=O
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Synonyms
(S)-CGP52421
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
(S)-3-Hydroxy Midostaurin Related Classifications
HY-108263A Related Classifications
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