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

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

Angiogenesis

Bcl-2

Bcl-2

Cancer

Blood cancer

1448584-12-0

710.83

C43H42N4O6

99.5% (LCMS)

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