S55746 hydrochloride (C09-1169-719)

S55746 hydrochloride (BCL201 hydrochloride) is a potent, orally active and selective BCL-2 inhibitor, with a K i of 1.3 nM and a K d of 3.9 nM. S55746 hydrochloride (BCL201 hydrochloride) has antitumor activity with low toxicityIn VitroS55746 (0-1 μM) potently and selectively induces cell death. S55746 selectively induces apoptosis through BCL-2 inhibition in a BAX/BAK-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: H146 and RS4;11 cell lines. Concentration: 0, 0.1, 0.3 and 1 μM. Incubation Time: 72 hours. Result: Potently induced RS4;11 cell killing after 72 h of treatment with an IC 50 of 71.6 nM.In VivoS55746 is a highly efficacious and well-tolerated (even at doses up to 300 mg/kg) orally active BCL-2 inhibitor . S55746 (20-100 mg/kg, p.o.) inhibits xenograft growth in RS4;11 and Toledo models time- and dose-dependently . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female SCID/beige mice implanted subcutaneously with 3×10 6 Toledo or RS4;11 . Dosage: 20, 50, 100 mg/kg. Administration: Oral gavage daily for 7 consecutive days. Result: Induced significant anti-tumor activity time- and dose-dependently. Animal Model: SCID/beige female mice with RS4;11 tumor xenografts . Dosage: 25 and 100 mg/kg. Administration: Single oral gavage treatment. Result: Did not induce platelet loss in vivo at 25 and 100 mg/kg.Form:SolidIC50& Target:Bcl-2 1.3 nM (Ki) Bcl-xL 520 nM (Ki) Bcl-2 3.9 nM (Kd) Bcl-xL 186 nM (Kd). Specification: 0.98 Molecular Formula: C43H43ClN4O6 Molecular Weight: 747.28 PubChem CID: 71654876 Isomeric SMILES: C1CCN2C(=C(C=C2C3=CC4=C(C=C3C(=O)N5CC6=CC=CC=C6C[C@H]5CN7CCOCC7)OCO4)C(=O)N(C8=CC=CC=C8)C9=CC=C(C=C9)O)C1