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Art. -Nr.: HY-184342

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SYC-2863

SYC-2863 is a CRBN-recruiting PROTAC degrader that selectively degrades ENL (MLLT1), with an ENL DC₅₀ of 45 nM in MV4;11 cells. SYC-2863 inhibits the proliferation of MLL-rearranged leukemia and multiple myeloma cells. After degrading intracellular ENL, SYC-2863 dose-dependently downregulates the transcription levels of MYC and its downstream target genes, blocking the MYC-mediated malignant proliferation pathway. SYC-2863 can be used in studies related to MLL-rearranged leukemia and multiple myeloma.

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Formel: C₄₂H₄₇N₉O₅
Molecular Weight:757.88

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Please store the product under the recommended conditions in the Certificate of Analysis.

SYC-2863 Chemical Structure

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Beschreibung

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In Vitro

SYC-2863 (compound 14) (0-1000 nM; 24 h) potently and selectively degrades ENL (DC₅₀ = 45 nM, D_max = 97%) without altering AF9 levels in MV4;11 cells^[1].
SYC-2863 selectively inhibits proliferation of Molm-13 (EC₅₀ = 0.13 μM) and MV4;11 (EC₅₀ = 2.1 μM) MLL-rearranged leukemia cells, with weaker activity against RPMI-8226 multiple myeloma cells and no activity against HeLa solid tumor cells^[1].
SYC-2863 (2 μM; 0-60 min) undergoes rapid NADPH-dependent metabolic degradation in human liver microsomes, with an in vitro half-life of 11.6 minutes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

Molecular Weight 757.88
Formel C₄₂H₄₇N₉O₅
SMILES

O=C1CCC(N2C(C(C=CC=C3NCCCCCCCCN4C(C=CC(C(NC5=CC(NC(CN6[C@@H](C)CCC6)=C7)=C7C=N5)=O)=C8)=C8C=N4)=C3C2=O)=O)C(N1)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Li X, et al.. Synthesis, structure-activity relationships, antitumor activities and mechanistic studies of ENL-degrading compounds. European journal of medicinal chemistry. 2026 May 19;316:118989. [Content Brief]

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Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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SYC-2863

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SYC-2863 Related Classifications

HY-184342 Related Classifications