BMS-202

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BMS-202 是 PD-1/PD-L1 相互作用的小分子抑制剂，在同质时间分辨荧光结合测定中 IC50 为 18 nM。

BMS-202 is a small molecule inhibitor of the PD-1/PD-L1 interaction with IC50 of 18 nM in a homogenous time-resolved fluorescence binding assay.

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.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.Cell Proliferation Assay Cell Line:SCC-3 or Jurkat cells Concentration:0-100 μM Incubation Time:4 days Result:Inhibited 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.

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. Animal Model:NOG-dKO mice (8-week-old) injected with SCC-3 cells Dosage:20 mg/kg Administration:Intraperitoneal injection; daily; for 9 days Result:Showed 41% growth inhibitory activity against humanized mouse-transplanted human lymphoma SCC-3 cells.

PD-1/PD-L1 inhibitor 2 | BMS202 | BMS 202

Immunology/Inflammation

PD-1/PD-L1

PD-1/PD-L1

Inflammation/Immunology

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1675203-84-5

419.5161

C25H29N3O3

>98% (HPLC)

DMSO: ≥ 30 mg/mL

CC(NCCNCC1=CC=C(OCC2=C(C)C(C3=CC=CC=C3)=CC=C2)N=C1OC)=O

Acetamide, N-[2-[[[2-methoxy-6-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]-3-pyridinyl]methyl]amino]ethyl]-

(-20℃)

With Ice Pack

≥ 2 years