BMS-1001

Description: BMS-1001 is a novel and potent small molecule inhibitor of the PD-1/PD-L1 protein protein interaction with IC50 value of 2.25 nM in cell free assays. It was first discovered by Bristol-Myers Squibb. Blockade of the PD-1/PD-L1 immune checkpoint pathway with monoclonal antibodies has provided significant advances in cancer treatment. The antibody-based immunotherapies carry a number of disadvantages such as the high cost of the antibodies, their limited half-life, and immunogenicity. Development of small-molecule PD-1/PD-L1 inhibitors that could overcome these drawbacks is slow because of the incomplete structural information for this pathway. The first chemical PD-1/PD-L1 inhibitors, BMS-1001 and its analogs, have been recently disclosed by Bristol-Myers Squibb.

References: J Med Chem. 2017 Jul 13; 60(13):5857-5867; Oncotarget. 2017 Aug 7; 8(42):72167-72181; WO/2015034820 A1

Related CAS#: 2113650-04-5 (HCl)