BCL-201 (S55746, Servier-1) is an orally bioavailable, potent and selective BH3-mimetic inhibitor of BCL-2 protein with a Ki of 1.3 nM, highly selective over BCL-XL (70- 400 fold), and no significant binding to MCL-1 and BFL-1 (BCL2A1/A1). BCL-201 induces hallmarks of apoptosis including externalization of phosphatidylserine, caspase-3 activation and PARP cleavage. Ex vivo, it induces apoptosis in the low nanomolar range in primary Chronic Lymphocytic Leukemia and Mantle Cell Lymphoma patient samples. Finally, BCL-201 (S55746) administered by oral route daily in mice demonstrated robust anti-tumor efficacy in two hematological xenograft models with no weight lost and no change in behavior.

KEYWORDS: BCL-201 dihydrochloride | BH3-mimetic inhibitor of BCL-2 protein | Servier 1 dihydrochloride | BCL201 | BCL 201 | S-55746 | S 55746 | CT-BCL201 | CAS [N.A.] | [1448584-12-0] | Non Selective | Bcl | Inhibitor | Proteins