S55746

Research use only, not for human use.

S55746 (BCL201, Servier-1) is a novel potent, selective, orally bioavailable inhibitor of BCL-2 with Ki of 1.3 nM.

S55746 (BCL201, Servier-1) is a novel potent, selective, orally bioavailable inhibitor of BCL-2 with Ki of 1.3 nM, 70- 400 fold selectivity over BCL-XL, on significant binding to MCL-1 and BFL-1; potently induces RS4;11 cell killing after 72 h of treatment with an IC50 of 71.6 nM, exhibits a much weaker activity in H146 (IC50 1.7 μM), a BCL-XL-dependent cell line; concentration-dependently disrupts the BCL-2/BAX complex in RS4;11 cells, selectively induces apoptosis through BCL-2 inhibition in a BAX/BAK-dependent manner; induces cell death in a panel of non-Hodgkin lymphoma cells; inhibits xenograft growth in RS4;11 and Toledo models.Blood Cancer Phase 1 Clinical.

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 IC50 of 71.6 nM.

Animal Model:Female SCID/beige mice implanted subcutaneously with 3×106 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.

BCL201 | BCL-201 | S 55746 | S-55746 | Servier-1

Angiogenesis

Bcl-2

Bcl-2

Cancer

Blood cancer

1448584-12-0

710.831

C43H42N4O6

>98% (HPLC)

DMSO : 50 mg/mL 70.34 mM; H2O : < 0.1 mg/mL

O=C(C1=C2CCCCN2C(C3=C(C(N4CC5=C(C=CC=C5)C[C@H]4CN6CCOCC6)=O)C=C(OCO7)C7=C3)=C1)N(C8=CC=C(O)C=C8)C9=CC=CC=C9

(S)-N-(4-hydroxyphenyl)-3-(6-(3-(morpholinomethyl)-1,2,3,4-tetrahydroisoquinoline-2-carbonyl)benzo[d][1,3]dioxol-5-yl)-N-phenyl-5,6,7,8-tetrahydroindolizine-1-carboxamide

(-20℃)

With Ice Pack

≥ 2 years