RGNCY-0119 (ECPU-0001 BCL-2 inhibitor)

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ECPU-0001 is a potent BCL-2 targeting agent(as confirmed by molecular docking) with effective anticancer activity.  ECPU-0001 exerts a significant cytotoxic effect against lung adenocarcnima cells (A459, IC50=1.779µM).  ECPU-0001 induces apoptosis in A459 cells by targeting BC:L-2.  The administration of ECPU-0001 to to tumor xenograft models resulted in an inhibition of tumor growth without exerting severe toxicity.  Therefore, ECPU-0001 may provide a new avenue for lung adenocarcinoma therapy.

Systematic Name: 1-(9-ethyl-9H-carbazol-3-yl)-3-(2-(4-(furan-2-carbonyl)piperazin-1-yl)ethyl)urea

SMILES:  CCN1C2=CC=CC=C2C3=C1C=CC(NC(NCCN4CCN(C(C5=CC=CO5)=O)CC4)=

                 O)=C3

Formula:   C26H29N5O3

Mol Wt:  459.55