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Cat. No.: 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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Formule: C₄₂H₄₇N₉O₅
Masse moléculaire:757.88

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SYC-2863 Chemical Structure

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Description

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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

Masse moléculaire 757.88
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[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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SYC-2863

Voir tous les produits spécifiques à Isoform PROTACs

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Activité biologique

Chemical Information

Pureté et documentation

Références

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SYC-2863 Related Classifications

HY-184342 Related Classifications