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PD-1/PD-L1

PD-1 inhibitors and PD-L1 inhibitors are a group of checkpoint inhibitor anticancer drugs that block the activity of PD-1 and PDL1 immune checkpoint proteins present on the surface of cells. Immune checkpoint inhibitors are emerging as a front-line treatment for several types of cancer.

  • PD-1/PD-L1-IN-10
    T96162487550-41-2
    PD-1/PD-L1-IN-10 is an orally active PD-1/PD-L1 inhibitor (IC50 of 2.7 nM) with potent anticancer efficacy.
    • $44
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  • Nivolumab
    T9907946414-94-4
    Nivolumab (anti-PD-1) is a genetically engineered fully human immunoglobulin Ig) G4 monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed death-1PD-1PCD-1) with immune checkpoint inhibitory and antineoplastic activities.
    • $182
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  • Pembrolizumab
    T99081374853-91-4
    Pembrolizumab is a humanized monoclonal antibody inhibiting the PD-1 receptor and the first in the class of agents called the HER2 dimerization inhibitors that impairs the ability of HER2 to bind to other members of the HER family.
    • $218
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  • Atezolizumab
    T99021380723-44-3
    Atezolizumab anti-PD-L1) is a fully humanized IgG1 monoclonal antibody that blocks the interaction of PD-L1 with both PD-1 and B7.1 but not the interaction of PD-L2 with PD-1.
    • $229
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  • BMS202 hydrochloride (1675203-84-5(free base))
    T46962089334-95-0
    BMS202 hydrochloride (1675203-84-5(free base)) (PD-1/PD-L1 inhibitor 2 hydrochloride) is a small-molecule PD-1/PD-L1 interaction inhibitor (IC50: 18 nM). Biophysical studies demonstrate that BMS202 binds directly to PD-L1. Binding of BMS202 promotes PD-L1 dimerisation and blocks the PD-L1/ PD1 interaction.
    • $47
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  • PD-1-IN-22
    T123792349372-98-9In house
    PD-1-IN-22 is a potent programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction inhibitor(IC50 of 92.3 nM).
    • $117
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  • IMMH 010 maleate
    T839702541982-47-0In house
    IMMH 010 maleate (YPD-30 maleate) is an orally available programmed cell death ligand 1 inhibitor with potential antitumor activity for the study of neurological disorders and advanced malignant solid tumors.
    • $195
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  • ARB-272572 hydrochloride
    T839762377524-19-9In house
    ARB-272572 hydrochloride is a small molecule PD-L1 inhibitor with an IC50 value of 400 pM for PD-1/PD-L1 HTRF.ARB-272572 hydrochloride inhibits PD-1/PD-L1 cell signaling by inducing homologous interactions with PD-L1 proteins.
    • $195
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  • LSD1-IN-27
    T776352904571-94-2
    LSD1-IN-27 is a potent LSD1 inhibitor with an IC50 value of 13 nM.LSD1-IN-27 inhibited the stemness and migration of gastric cancer cells.LSD1-IN-27 inhibited the expression of PD-L1 in BGC-823 and MFC cells.LSD1-IN-27 potentiated the T-cell immune response against gastric cancer.
    • $195
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  • AUNP-12 acetate
    TP1076L
    AUNP-12 acetate is a polypeptide inhibitor of PD-1 that is equivalent to PD-1 and PD-2 in inhibiting lymphocyte proliferation and effector fuction, in addition to immune activation and antitumor activity.
    • $116
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  • BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride
    T40111L2691796-83-3In house
    BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride is a resorcinol di-Ph ether scaffold-based programmed cell death-1 (PD-1)/programmed cell death ligand 1 (PD-L1) inhibitor that inhibits the PD-1/PD-L1 interaction with an IC50 of 39.2 nM.BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride contains the target protein PD-1/PD-L1 ligand and PROTAC linker.BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride can be used to synthesize PROTAC linker. BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride can be used to synthesize PROTAC PD-1/PD-L1 degrader-1. BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride has anticancer activity. BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride can be used as a diluent for the preparation of tablets for direct compression.
    • $222
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  • PD-1-IN-17
    T123771673560-66-1In house
    PD-1-IN-17 is an inhibitor of programmed cell death-1 (PD-1). PD-1-IN-17 inhibits 92% splenocyte proliferation at 100 nM.
    • $110
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  • PD-1/PD-L1-IN-9
    T96512628506-54-5In house
    PD-1/PD-L1-IN-9, with an IC50 of 3.8 nM, is a potent and orally active inhibitor of the PD-1/PD-L1 interaction. It enhances the immune cells' ability to kill tumor cells and demonstrates significant antitumor activity in vivo in a CT26 mouse model.
    • $55
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  • BMS-1
    T36551675201-83-8
    BMS-1 (PD-1/PD-L1 inhibitor 1) is an inhibitor of the PD1-PD-L1 protein-protein interaction. It also acts as an immunomodulator. Programmed death ligand 1 (PD-L1) is a protein in humans that is encoded by the CD274 gene and the upregulation of PD-L1 allows Ys to evade the host immune system. High tumor expression of PD-L1 was associated with increased tumor aggressiveness and a 4.5-fold increased risk of death.
    • $48
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  • BMS-202
    T31461675203-84-5
    BMS-202 (PD1-PDL1 inhibitor 2) is an inhibitor of the PD-1 (Programmed death- 1) /PD-Ll (Programmed death-ligand 1) protein/protein interaction.
    • $57
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  • Tomivosertib
    T34681849590-01-7
    Tomivosertib (eFT508) is a potent, highly selective MNK1 and MNK2 inhibitor with IC50 value of 1-2 nM.
    • $59
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  • Anti-Mouse PD-1 Antibody (RMP1-14)
    T78269
    RMP1-14 is an IgG1-like immunoglobulin and anti-Mouse PD-1 antibody that blocks PD-1/PD-L1 signaling.
    • $99
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  • Anti-Mouse PD-L1 Antibody (10F.9G2)
    T78270
    Anti-Mouse PD-L1 Antibody is a rat-derived IgG2b monoclonal antibody that inhibits mouse PD-L1.
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  • ASC-69
    T829601216665-50-7
    ASC-69 (APY69) is a promising potent inhibitor of the PD-1/PD-L1 signaling pathway, classified as a small-molecule compound [1].
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  • Reozalimab
    T806172445259-99-2
    Rezilimab is a bispecific antibody that targets PD-1/PD-L1 and mediates antibody-dependent cell cytotoxicity (ADCC) in cancer research [1] [2].
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  • Eciskafusp alfa
    T825082649758-52-9
    Eciskafusp alfa, a cis-targeted IL2v immunocytokine, acts on programmed cell death 1 (PDCD1, commonly known as PD-1), preferentially targeting antigen-specific stem-like PD-1+ TCF-1+ CD8+ T cells to differentiate into a more effective effector population. This compound is applicable in the study of cancer and chronic infections [1].
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  • CAY10678
    T383691268709-57-4
    CAY10678 is an mPGES-1 inhibitor that inhibits PD-1.CAY10678 reduces collagen deposition and T-cell depletion, and may be used to study melanoma.CASHIPS
    • $48
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  • Rosnilimab
    T806192412764-40-8
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  • Pidilizumab
    T814611036730-42-3
    Pidilizumab (CT-011), a humanized IgG1κ anti-PD-1 monoclonal antibody, serves as a DLL1 antagonist with potential applications in researching hematologic malignancies [1].
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  • Lipustobart
    T819282639481-06-2
    Lipustobart is an IgG4-kappa humanized monoclonal antibody targeting PDCD1 (programmed cell death 1, PD1, PD-1, CD279), with immunostimulant and antineoplastic activity [1].
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  • Danburstotug
    T826132307144-65-4
    Danburstotug (IMC-001), an immunostimulant and antineoplastic [1], is a humanized IgG1-lambda monoclonal antibody targeting CD274 (PDL1, B7 homologue 1, B7H1).
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  • Visugromab
    T808632556646-63-8
    Visugromab, a GDF-15 neutralizing IgG4 monoclonal antibody (mAb), demonstrates potent efficacy in treating PD-1/PD-L1 relapsed/refractory metastatic solid tumors [1].
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  • Sasanlimab
    T806112206792-50-7
    Sasanlimab (PF-06801591), a humanized IgG4-κ antibody, selectively targets PD-1 and is primarily produced in Chinese Hamster Ovary (CHO) cells [1].
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  • Spartalizumab
    T770751935694-88-4
    Spartalizumab (PDR001) is a humanized immunoglobulin 4 monoclonal antibody that selectively binds to PD-1 at low concentrations and shows high activity. Spartalizumab blocks the interaction with PD-L1 and PD-L2, and can be used to study undifferentiated thyroid cancer (ATC).
    • $178
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  • Durvalumab
    T111261428935-60-7
    Durvalumab (MEDI 4736) is a humanized monoclonal antibody targeting PD-L1. It can block the interaction of PD-L1 with PD-1 and CD80, with IC50 values of 0.1 and 0.04 nM, respectively. Durvalumab is often used in combination with platinum-based compounds for the treatment of non-small cell lung cancer and advanced hepatocellular carcinoma cells.
    • $228
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  • LSD1-IN-24
    T678714734-59-2
    LSD1-IN-24 is a selective and potent LSD1 inhibitor with an IC50 value of 0.247 μM.LSD1-IN-24 induces PD-L1 expression and enhances the T cell killing response, and can be used in cancer-related diseases.
    • $73
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  • Feladilimab
    T774332252518-85-5
    Feladilimab (GSK3359609) is an IgG4 monoclonal antibody that is an ICOS agonist. Feladilimab binds to ICOS-expressing T cells, induces IFNγ, and increases PD-1/L1 expression. Feladilimab has anti-tumor activity and can be used to study cancer.
    • $247
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  • PD-1/PD-L1-IN-32
    T79576
    PD-1/PD-L1-IN-32 (compound A56) is a potent inhibitor of PD-1/PD-L1, displaying pronounced anticancer activity with an IC50 value of 2.4 nM. It effectively suppresses tumor growth in the hPD-L1 MC38 humanized mouse model and exhibits negligible toxicity to the mice's normal functions [1].
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  • PD-1/PD-L1-IN-27
    T726802891831-47-1
    PD-1/PD-L1-IN-27 is a potent inhibitor of PD-1/PD-L1, exhibiting an IC50 of 134 nM and demonstrating antitumor effects with minimal T cell cytotoxicity. It activates CD8+ T cells and mitigates T cell exhaustion [1].
    • $1,520
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  • Fraxinellone
    T6S007128808-62-0
    1. Fraxinellone significantly reduced weight loss and diarrhea in mice and alleviated the macroscopic and microscopic signs of the disease. 2. Fraxinellone exhibited a variety of insecticidal activities including feeding-deterrent activity, inhibition of growth, and larvicidal activity. 3. Fraxinellone has effect in the midgut metabolism of Mythimna separata (M. separata), via protease (especially the weak alkaline trypsin-like enzyme), carboxylesterase and glutathione S-transferase.
    • $66
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  • PD-L1-IN-3
    T793142953044-29-4
    PD-L1-IN-3 (Compound 4a) functions as an inhibitor targeting the PD-1/PD-L1 axis, with an IC50 value of 4.97nM for PD-L1 inhibition and an EC50 value of 2.70 μM for Jurkat T cell modulation. It antagonizes the PD-1/PD-L1 interaction by binding to the PD-L1 dimer, obstructing PD-1 signaling. This compound is utilized in research pertaining to lung cancer and melanoma [1].
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  • LP23
    T79705
    LP23, a non-arylmethylamine PD-1/PD-L1 inhibitor (IC 50: 16.7 nM), exhibits anti-tumor activity through the restoration of immune cell function in HepG2/Jurkat T cells and induction of HepG2 cell death. Additionally, LP23 demonstrates in vivo efficacy in the B16-F10 tumor model (TGI=88.6% at 30 mg/kg) [1].
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  • PD-1/PD-L1-IN-33
    T796432975602-78-7
    PD-1/PD-L1-IN-33 (Compound N11), a PD-1/PD-L1 inhibitor, effectively impedes the interaction between PD-1 and PD-L1 with an IC50 of 6.3 nM. By doing so, it enhances T-cell proliferation, activation, and infiltration within tumor environments, exhibiting immunomodulatory and anticancer properties [1].
    • $1,670
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  • PD-1/PD-L1-IN-31
    T78755
    PD-1/PD-L1-IN-31 is a potent inhibitor of PD-1/PD-L1 (IC50=2.2 nM) that enhances IFN-γ secretion and activates the immune response of peripheral blood mononuclear cells (PBMCs), resulting in the inhibition of tumor cells [1].
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  • INCB086550
    T368992230911-59-6
    INCB086550 (PD-1/PD-L1-IN-8) (example 24) is a PD-1/PD-L1 inhibitor, with an IC50 <= 10 nM.
    • $148
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  • PD-1/PD-L1-IN-26
    T726682966090-78-6
    PD-1/PD-L1-IN-26 (Compound II-14) is a potent PD-1/PD-L1 inhibitor, demonstrating an IC50 of 0.0380 μM. It enhances the immune microenvironment by facilitating CD4+ T cell infiltration into tumor tissues, indicating potential use in cancer research [1].
    • $1,520
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  • BMS-1001 hydrochloride
    T105652113650-04-5
    BMS-1001 hydrochloride is an orally active inhibitor of human PD-1/PD-L1 immune checkpoint with low-toxicity in cells.BMS-1001 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes. BMS-1001 is capable of alleviating the PD-1/PD-L1 immune checkpoint-mediated exhaustion of Jurkat T-lymphocytes.
    • $55
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  • Sintilimab (anti-PD-1)
    T353942072873-06-2
    Sintilimab (IBI308) is a humanized IgG4 monoclonal antibody with significant anti-tumor activity that restores endogenous anti-tumor T-cell responses by binding to PD-1 and thereby blocking the interaction of PD-1 with its ligands (PD-L1 and PL-L2).Sintilimab is used in combination with other compounds for the treatment of classical Hodgkin's lymphoma, non-cellular lung cancer and esophageal cancer. Sintilimab is used in combination with other compounds to treat classical Hodgkin's lymphoma, non-small cell lung cancer and esophageal cancer.
    • $163
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  • BMS-1166
    T56971818314-88-3
    BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor.
    • $89
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  • PDL-1 cpd 10
    T93592767424-13-3
    PDL-1 cpd 10 is a novel small molecule PD-L1 inhititor.
    • $84
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  • Acrixolimab
    T805822506324-29-2
    Acrixolimab is a humanized IgG4-κ monoclonal antibody that selectively targets PD-1 [1] [2].
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  • PD-L1-IN-2
    T780532894733-91-4
    PD-L1-IN-2, a Naamidine J derivative, serves as a promising antineoplastic immunomodulator by hindering PD-L1 activity. In vivo studies indicate that it suppresses PD-L1 expression and amplifies tumor-infiltrating T-cell response, thus exerting anticancer effects. This compound is particularly utilized in the investigation of colorectal cancer [1].
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  • SWS1
    T795282922115-32-8
    SWS1, a d-(+)-biotin-conjugated PD-L1 inhibitor (IC50: 1.8 nM), displays anticancer activity by augmenting tumor-infiltrating lymphocytes and demonstrating anti-tumor efficacy, as evidenced by a 66.1% tumor growth inhibition (TGI=66.1%) in the B16-F10 mouse model [1].
    • $1,820
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  • PD-1/PD-L1-IN-NP19
    T369002377916-66-8
    PD-1/PD-L1-IN-NP19, a PD-1/PD-L1 inhibitor, exhibits an IC50 of 12.5 nM against the human PD-1/PD-L1 interaction, potentially activating the tumor immune microenvironment and contributing to its antitumor effects[1].
    • $376
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  • BMS-8
    T268591675201-90-7
    BMS-8 is a novel inhibitor of the PD-1/PD-L1 interaction (IC50: 7.2 μM) by binding directly to PD-L1 and inducing the formation of PD-L1 homodimers.
    • $33
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