SKU : MC530493
CAS Number : 1675203-84-5
Molecular Formula : C25H29N3O3 | Molecular Weight : 419.52
Quote RequestPurity | NLT 98% |
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Storage | at 20ºC 2 years |
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Chemical Name | BMS-202 |
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CAS Number | 1675203-84-5 |
Molecular Formula | C25H29N3O3 |
Molecular Weight | 419.52 |
BMS-202 is a potent and nonpeptidic PD-1/PD-L1 complex inhibitor with an IC50 of 18 nM and a KD of 8 μM. BMS-202 binds to PD-L1 and blocks human PD-1/PD-L1 interaction. BMS-202 has antitumor activity[1][2]. IC50 & Target: IC50: 18 nM (PD-1/PD-L1)[1]
KD: 8 μM (PD-1/PD-L1)[1] In Vitro: BMS-202 (0-100 μM; 4 days; SCC-3 or Jurkat cells) treatment inhibits the proliferation of strongly PD-L1-positive SCC-3 cells (IC50 of 15 μM) and anti-CD3 antibody-activated Jurkat cells (IC50 10 μM) in vitro[2].
BMS-202 selectively induces thermal stabilization of PD-L1. BMS-202 induces dimerization of PD-L1 in solution.BMS-202 is located at the center of the homodimer filling a deep hydrophobic pocket contributing multiple additional interactions between the monomers. BMS-202 interacts with both PD-L1 molecules using hydrophobic surfaces physiologically involved in the PD-1/PD-L1 interaction[1]. In Vivo: BMS-202 (20 mg/kg; intraperitoneal injection; daily; for 9 days; NOG-dKO mice) treatment shows a clear antitumor effect compared with the controls, in humanized MHC- dKO NOG mice[2].
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