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BCL-201 (S55746)
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 (ref.1).
Catalog NO: CT-BCL201
Synonym: BCL201, S-55746, SERVIER-1
CAS NO: 1448525-91-4
Mol. Formula: C43H42N4O6
MW: 710.8 (refer to Certificate of Analysis, batch-specific)
** in vivo quality product, >99.5% Pure by achiral and chiral HPLCs. Dihydrochloride, validated by a spot-on Quantitative Elemental Analysis. In stock, prompt.