A PD-1/PD-L1 interaction inhibitor
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LH1307

Item No. 28728

Technical Information
Formal Name
N,N'-(((((((2,2'-dimethyl-[1,1'-biphenyl]-3,3'-diyl)bis(methylene))bis(oxy))bis(2-((5-cyanopyridin-3-yl)methoxy)-5-methyl-4,1-phenylene))bis(methylene))bis(azanediyl))bis(ethane-2,1-diyl))diacetamide
CAS Number
2375720-38-8
Molecular Formula
C54H58N8O6
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 25 mg/mlDMSO: 25 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.3 mg/mlEthanol: 10 mg/ml
SMILES
CC1=C(COC2=C(C)C=C(CNCCNC(C)=O)C(OCC3=CN=CC(C#N)=C3)=C2)C=CC=C1C4=C(C)C(COC5=CC(OCC6=CN=CC(C#N)=C6)=C(CNCCNC(C)=O)C=C5C)=CC=C4
InChi Code
InChI=1S/C54H58N8O6/c1-35-17-47(29-57-13-15-61-39(5)63)53(65-31-43-19-41(23-55)25-59-27-43)21-51(35)67-33-45-9-7-11-49(37(45)3)50-12-8-10-46(38(50)4)34-68-52-22-54(66-32-44-20-42(24-56)26-60-28-44)48(18-36(52)2)30-58-14-16-62-40(6)64/h7-12,17-22,25-28,57-58H,13-16,29-34H2,1-6H3,(H,61,63)(H,62,64)
InChi Key
RNCINFJGGSQEHN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    LH1307 is an inhibitor of the interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 that has an IC50 value of 3 nM in a homologous time-resolved fluorescence (HTRF) assay.1 It increases the activation of Jurkat cells expressing PD-1 in co-culture with U2OS or CHO cells expressing PD-L1 (EC50s = 79 and 763 nM, respectively, in reporter assays).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Basu, S., Yang, J., Xu, B., et alDesign, synthesis, evaluation, and structural studies of C2-symmetric small molecule inhibitors of programmed cell death-1/programmed death-ligand 1 protein-protein interaction. J. Med. Chem. 62(15), 7250-7263 (2019).