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Results for "

PD-1/PD-L1 blockade

" in MedChemExpress (MCE) Product Catalog:

By Targets:	PD-1/PD-L1 (7) c-Kit (2) CD3 (1) DGK (1) Discoidin Domain Receptor (2) FLT3 (3) IKK (1) Interleukin Related (2) Phosphatase (1) TNF Receptor (2) Toll-like Receptor (TLR) (3) Trk Receptor (2) VEGFR (3)
By Research Areas:	Cancer (14) Inflammation/Immunology (7)

Inhibitors & Agonists

Inhibitory Antibodies

Targets Recommended: PD-1/PD-L1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P9902A

Pembrolizumab (anti-PD-1) 5 Publications Verification MK-3475 (anti-PD-1); Lambrolizumab (anti-PD-1)	PD-1/PD-L1	Cancer
Pembrolizumab (anti-PD-1) is a humanized IgG4 antibody and *PD-1* inhibitor. Pembrolizumab produces *PD-1* blockade, preventing PD-L1 and PD-L2 from connecting to *PD-1. This avoids the uncontrolled regulation of T cells on cells that normally express PD-1* .

HY-16961

Sitravatinib Maximum Cited Publications 6 Publications Verification MGCD516; MG-516	VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor	Inflammation/Immunology Cancer
Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC₅₀s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .

HY-128679

TBK1/IKKε-IN-5	IKK	Cancer
TBK1/IKKε-IN-5 (compound 1) is an orally active TBK1 and IKKε dual inhibitor, with IC₅₀ values of 1 and 5.6 nM, respectively. TBK1/IKKε-IN-5 enhances the blockade response to *PD-1* and induces immune memory in rats when combines with anti-PD-L1. TBK1/IKKε-IN-5 can be used in cancer research, especially in tumour immunity .

HY-P991740

IBI-363	PD-1/PD-L1 Interleukin Related	Cancer
IBI-363 is a *PD-1/IL-2* bispecific antibody with functions of blocking the PD-1/PD-L1 pathway and activating the IL-2 pathway. The IL-2 arm of IBI-363 retains affinity for IL-2Rα but attenuates binding ability to IL-2Rβ and IL-2Rγ to reduce toxicity. The PD-1 binding arm of IBI-363 enables PD-1 blockade and selective delivery of IL-2. IBI-363 can be used in cancer research, such as non-small cell lung cancer .

HY-P99916

Emirodatamab AMG-427	FLT3 CD3 TNF Receptor	Inflammation/Immunology Cancer
Emirodatamab (AMG-427) is a bispecific T-cell engager (BiTE). Emirodatamab simultaneously binds FLT3 on the surface of acute myeloid leukemia (AML) cells and CD3 on the surface of T cells, thereby precisely recruiting immune effector cells to tumor sites. Emirodatamab potently induces T cell activation, secretion of proinflammatory cytokines (such as IFNγ, TNFα), and specific cytotoxicity, effectively lysing FLT3-positive tumor cells and inhibiting their growth. Emirodatamab not only significantly prolongs survival in mouse xenograft models and eliminates diseased cells in primates, but also exhibits a synergistic enhancement effect when combined with *PD-1* blockade therapy. Emirodatamab is used in studies of acute myeloid leukemia, especially relapsed or refractory cases .

HY-144501

D18	Toll-like Receptor (TLR) PD-1/PD-L1	Inflammation/Immunology Cancer
D18 is an immune modulator. D18 acts as a TLR7/8 dual agonist (EC₅₀ = 24 nM for hTLR7 and 10 nM for hTLR8, respectively). D18 increases *PD-L1* expression through epigenetic regulation, thus sensitizing tumors to PD-1/PD-L1 blockade. D18 is a ADC cytotoxin uesd for the systhesis of ADC HE-S2 (HY-144497). D18 has strong immune activation and anti-tumor activity. D18 commonly used in cancer research, such as colon cancer .

HY-P991193

NGM-438	TNF Receptor	Cancer
NGM-438 is a humanized monoclonal antibody antagonist of LAIR1, with a K_a of 0.26 nM for human LAIR1 and 4.28 nM for cynomolgus monkey LAIR1. NGM-438 blocks the binding of LAIR1 to its Collagen ligand and antagonizes the Collagen-induced LAIR1 signaling pathway. NGM-438 reverses FcγR signaling inhibition in myeloid cells, induces dendritic cells to secrete TNFα, promotes T cell proliferation, and triggers myeloid inflammation and allogeneic T cell responses. NGM-438 sensitizes refractory mouse lung cancer to *PD-1* blockade, increases the content of intratumoral CD8 ⁺ T cells and the expression of inflammatory genes. NGM-438 is applicable to research related to solid tumors, refractory solid tumors and non-small cell lung cancer .

HY-155847

LYP-IN-3	Phosphatase PD-1/PD-L1	Inflammation/Immunology Cancer
LYP-IN-3 is a selective, orally active and reversible lymphoid-tyrosine phosphatase (LYP) inhibitor (IC₅₀ = 2.55 μM, Ki = 0.93 μM). D34 exhibits high selectivity of PTP1B, PTPN12, PTPN5 and SSH2. LYP-IN-3 regulates the T-cell receptor (TCR) signaling by specifically inhibiting LYP. LYP-IN-3 does not significantly inhibit MC38 cell viability; its anti-tumor effect stems from immune regulation. LYP-IN-3 can significantly upregulate *PD-L1* or *PD-1* expression in different immune cells. LYP-IN-3 facilitates T-cell infiltration and enhances T-cell functions. LYP-IN-3 synergizes with *PD-L1* blockade can significantly improve colorectal tumor regression. LYP-IN-3 can be used for the study of colorectal cancer .

HY-16961A

Sitravatinib malate MGCD516 malate; MG-516 malate	VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor	Inflammation/Immunology Cancer
Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC₅₀s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .

HY-P991738

LM-299	PD-1/PD-L1 VEGFR	Cancer
LM-299 is a *PD-1/VEGF* bispecific antibody. LM-299 achieves its dual binding activity through the effective binding of the anti-VEGF-A antibody at the fab end to human VEGF-A, coupled with the blockade of the PD-1/PD-L1 pathway by the anti-PD-1 antibody at the-Fc end. LM-299 can be used for the study of non-small cell lung cancer (NSCLC).

HY-153543

TLR7/8 agonist 8	Toll-like Receptor (TLR)	Cancer
TLR7/8 agonist 8 (compound 24m) is a potent toll-like receptor 7/8 (TLR7/8) dual agonist, with EC₅₀s of 27 and 12 nM for hTLR7 and hTLR8, respectively. TLR7/8 agonist 8 can improve the antitumor activity of PD-1/PD-L1 blockade .

HY-163844

PD-1/PD-L1-IN-49	PD-1/PD-L1	Inflammation/Immunology Cancer
PD-1/PD-L1-IN-49 (compound 1c) is a potent inhibitor of PD-1/PD-L1, with the IC₅₀ of 77 nM. PD-1/PD-L1-IN-49 activates Jurkat T cells, reflecting successful blockade of the PD-1/PD-L1 immune checkpoint .

HY-161818

LLW-018	PD-1/PD-L1	Inflammation/Immunology
LLW-018 is a potent *PD-1/PD-L1* inhibitor with an IC₅₀ value of 2.61 nM. LLW-018 can interrupt PD-1/PD-L1 interaction with an IC₅₀ value of 0.88 μM by cell-based PD-1/PD-L1 blockade bioassays. LLW-018 has the potential for immunotherapy research .

HY-153544

TLR7/8 agonist 9	Toll-like Receptor (TLR)	Cancer
TLR7/8 agonist 9 (Compound 25a) is a TLR7/8 agonist, with EC₅₀s of 40 nM and 23 nM for hTLR7/8. TLR7/8 agonist 9 has anti-tumor activity and improves the antitumor activity of PD-1/PD-L1 blockade. TLR7/8 agonist 9 can be used for research of cancer immunotherapy .

HY-183539

INCB191358	DGK Interleukin Related	Cancer
INCB191358 is a selective and orally active inhibitor of diacylglycerol kinase α/ζ/ι (DGKα/ζ/ι ) with IC₅₀ values of 0.12, 0.36 and 0.36 nM. INCB191358 induces antigen-dependent T-cell activation, induces IL-2 production and enhances antitumor efficacy in combination with PD-1 blockade. INCB191358 can be used for the research of cancer, such as colon carcinoma .

Cat. No.	Product Name	Target	Research Area	Image

HY-P9902A

Pembrolizumab (anti-PD-1) 5 Publications Verification MK-3475 (anti-PD-1); Lambrolizumab (anti-PD-1)	PD-1/PD-L1	Cancer
Pembrolizumab (anti-PD-1) is a humanized IgG4 antibody and *PD-1* inhibitor. Pembrolizumab produces *PD-1* blockade, preventing PD-L1 and PD-L2 from connecting to *PD-1. This avoids the uncontrolled regulation of T cells on cells that normally express PD-1* .

HY-P991740

IBI-363	PD-1/PD-L1 Interleukin Related	Cancer
IBI-363 is a *PD-1/IL-2* bispecific antibody with functions of blocking the PD-1/PD-L1 pathway and activating the IL-2 pathway. The IL-2 arm of IBI-363 retains affinity for IL-2Rα but attenuates binding ability to IL-2Rβ and IL-2Rγ to reduce toxicity. The PD-1 binding arm of IBI-363 enables PD-1 blockade and selective delivery of IL-2. IBI-363 can be used in cancer research, such as non-small cell lung cancer .

HY-P99916

Emirodatamab AMG-427	FLT3 CD3 TNF Receptor	Inflammation/Immunology Cancer
Emirodatamab (AMG-427) is a bispecific T-cell engager (BiTE). Emirodatamab simultaneously binds FLT3 on the surface of acute myeloid leukemia (AML) cells and CD3 on the surface of T cells, thereby precisely recruiting immune effector cells to tumor sites. Emirodatamab potently induces T cell activation, secretion of proinflammatory cytokines (such as IFNγ, TNFα), and specific cytotoxicity, effectively lysing FLT3-positive tumor cells and inhibiting their growth. Emirodatamab not only significantly prolongs survival in mouse xenograft models and eliminates diseased cells in primates, but also exhibits a synergistic enhancement effect when combined with *PD-1* blockade therapy. Emirodatamab is used in studies of acute myeloid leukemia, especially relapsed or refractory cases .

HY-P991193

NGM-438	TNF Receptor	Cancer
NGM-438 is a humanized monoclonal antibody antagonist of LAIR1, with a K_a of 0.26 nM for human LAIR1 and 4.28 nM for cynomolgus monkey LAIR1. NGM-438 blocks the binding of LAIR1 to its Collagen ligand and antagonizes the Collagen-induced LAIR1 signaling pathway. NGM-438 reverses FcγR signaling inhibition in myeloid cells, induces dendritic cells to secrete TNFα, promotes T cell proliferation, and triggers myeloid inflammation and allogeneic T cell responses. NGM-438 sensitizes refractory mouse lung cancer to *PD-1* blockade, increases the content of intratumoral CD8 ⁺ T cells and the expression of inflammatory genes. NGM-438 is applicable to research related to solid tumors, refractory solid tumors and non-small cell lung cancer .

HY-P991738

LM-299	PD-1/PD-L1 VEGFR	Cancer
LM-299 is a *PD-1/VEGF* bispecific antibody. LM-299 achieves its dual binding activity through the effective binding of the anti-VEGF-A antibody at the fab end to human VEGF-A, coupled with the blockade of the PD-1/PD-L1 pathway by the anti-PD-1 antibody at the-Fc end. LM-299 can be used for the study of non-small cell lung cancer (NSCLC).

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