A PD-1/PD-L1 interaction inhibitor
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ARB-272572

Item No. 42547

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N,N′-(2,2′-dimethyl[1,1′-biphenyl]-3,3′-diyl)bis[5-[[(2-hydroxyethyl)amino]methyl]-2-pyridinecarboxamide
CAS Number
2368182-63-0
Molecular Formula
C32H36N6O4
Formula Weight
568.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C(C1=NC=C(CNCCO)C=C1)NC2=CC=CC(C3=C(C)C(NC(C4=NC=C(CNCCO)C=C4)=O)=CC=C3)=C2C
InChi Code
InChI=1S/C32H36N6O4/c1-21-25(5-3-7-27(21)37-31(41)29-11-9-23(19-35-29)17-33-13-15-39)26-6-4-8-28(22(26)2)38-32(42)30-12-10-24(20-36-30)18-34-14-16-40/h3-12,19-20,33-34,39-40H,13-18H2,1-2H3,(H,37,41)(H,38,42)
InChi Key
FZEPAZRIEAMJFE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $125

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    10 mg

    $220

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    25 mg

    $413

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    Product Description

    ARB-272572 is an inhibitor of the protein-protein interaction between programmed cell death protein 1 (PD-1) and PD-1 ligand (PD-L1; IC50 = 400 pM in a homogenous time-resolved fluorescence (HTRF) assay).1 It also inhibits the PD-1/PD-L1 interaction in a cell-based nuclear factor of activated T cells (NFAT) reporter assay (IC50 = 17 nM) and decreases cell surface levels of PD-L1 in primary human dendritic cells and B cells. ARB-272572 reduces cytomegalovirus antigen-induced IFN-γ production in a cytomegalovirus (CMV) recall assay using peripheral blood mononuclear cells (PBMCs) isolated from CMV seropositive patients (IC50 = 3 nM). In the presence of hepatitis B virus (HBV) peptides, it induces T cell proliferation and IFN-γ production in PBMCs isolated from patients with chronic HBV infection when used at a concentration of 500 nM. In vivo, ARB-272572 (10 mg/kg) reduces tumor volume and PD-L1 levels in CD45- tumor cells in a humanized MC-38 murine model of colon cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Park, J.-J., Thi, E.P., Carpio, V.H., et al. Checkpoint inhibition through small molecule-induced internalization of programmed death-ligand 1. Nat. Commun. 12(1), 1222 (2021).