2. Immunology/Inflammation GPCR/G Protein
  3. PD-1/PD-L1 CXCR
  4. PD-1/PD-L1-IN-63

PD-1/PD-L1-IN-63 is an orally active PD-1/PD-L1 inhibitor with an IC50 of 9.1 nM. PD-1/PD-L1-IN-63 blocks the PD-1/PD-L1 interaction, induces cancer cell death and inhibits tumor growth. PD-1/PD-L1-IN-63 can be used in the research of melanoma.

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PD-1/PD-L1-IN-63

PD-1/PD-L1-IN-63 Chemical Structure

CAS No. : 2691796-92-4

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PD-1/PD-L1-IN-63 Related Antibodies

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Description

PD-1/PD-L1-IN-63 is an orally active PD-1/PD-L1 inhibitor with an IC50 of 9.1 nM. PD-1/PD-L1-IN-63 blocks the PD-1/PD-L1 interaction, induces cancer cell death and inhibits tumor growth. PD-1/PD-L1-IN-63 can be used in the research of melanoma[1].

In Vitro

PD-1/PD-L1-IN-63 potently inhibits PD-1/PD-L1 protein interaction with an IC50 of 9.1 nM in an HTRF binding assay[1].
PD-1/PD-L1-IN-63 binds to both purified human PD-L1 (KD = 88.3 nM) and murine PD-L1 (KD = 174 nM) proteins with similar high affinities as measured by ITC[1].
PD-1/PD-L1-IN-63 (0.05-5 μM) binds dose-dependently to purified human PD-L1 (KD = 202 nM) and murine PD-L1 (KD = 471 nM) proteins as measured by SPR[1].
PD-1/PD-L1-IN-63 (37-1000 nM; 48 h) promotes HepG2 cell death in a dose-dependent manner in a HepG2/hPD-L1 and Jurkat/hPD-1 coculture cell model, increasing HepG2 mortality by 58.2% at 1000 nM[1].
PD-1/PD-L1-IN-63 (48 h) inhibits the proliferation of MCF-7, H1299, HeLa, HepG2, and Jurkat cells in vitro with IC50 values ranging from 2.3 μM to 4.1 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PD-1/PD-L1-IN-63 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: HepG2/hPD-L1, Jurkat/hPD-1
Concentration: 37, 111, 333, 1000 nM
Incubation Time: 48 h
Result: Promoted HepG2 cell death in a dose-dependent manner.
At 1000 nM, elevated the mortality rate of HepG2 cells by 58.2%, which was significantly higher than the positive control BMS-202.

Cell Viability Assay[1]

Cell Line: MCF-7, H1299, HeLa, HepG2, Jurkat
Concentration: /
Incubation Time: 48 h
Result: Had IC50 values of MCF-7 (3.2 μM), H1299 (3.7 μM), HeLa (4.1 μM), HepG2 (2.3 μM), Jurkat (2.8 μM).
Parmacokinetics
Species Dose Route AUC0-t AUC0-∞ MRT0-t MRT0-∞ T1/2 Tmax CL Vz Cmax F
Rat[1] 1 mg/kg i.v. 718.8 ng·h/mL 831.7 ng·h/mL 11.6 h 19.9 h 18.1 h 0.083 h 1.3 L/h/kg 31 L/kg 257.2 ng/mL /
Rat[1] 10 mg/kg p.o. 771.2 ng·h/mL 961.3 ng·h/mL 17.2 h 29.7 h 20.9 h 6.3 h 10.8 L/h/kg 310.2 L/kg 52.7 ng/mL 12 %
In Vivo

PD-1/PD-L1-IN-63 (50-100 mg/kg; i.g.; 14 days) exhibits potent dose-dependent antitumor activity in humanized PD-1 C57BL/6J mice inoculated with B16-F10 melanoma[1].
PD-1/PD-L1-IN-63 (50-100 mg/kg; i.g.; 14 days) does not induce cardiotoxicity or myelosuppression in healthy BALB/c mice when administered via oral gavage at doses of 50 or 100 mg/kg once daily for 14 days[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J-Pdcdem1(hPDCD1)/Smoc (n=5 per group)[1]
Dosage: 50 mg/kg; 100 mg/kg
Administration: i.g.; daily; 14 days
Result: Reduced tumor weight by 69.7% and tumor volume by 89.6% at 50 mg/kg compared to vehicle control.
Reduced tumor weight by 78.1% and tumor volume by 94.1% at 100 mg/kg compared to vehicle control.
Did not cause significant changes in body weight, spleen weight, or thymus weight compared to vehicle control.
Significantly increased tumor mRNA expression of CXCR3, CXCL9, and CXCL10 in the 100 mg/kg group.
Significantly reduced PD-L1 mRNA expression in both treatment groups.
Significantly increased tumor-infiltrating CD3+CD4+ and CD3+CD8+ T cell percentages in a dose-dependent manner in tumor tissue (but not spleen).
Significantly reduced tumor PD-L1 protein expression in both treatment groups.
Showed no morphological aberrations in liver and kidney via H&E staining compared to vehicle control.
Showed no significant differences in serum liver and kidney function markers compared to vehicle control.
Molecular Weight

696.11

Formula

C37H41Cl3N4O3
CAS No.
SMILES

N#CC1=CC=CC(COC2=CC(OCC3=CC=CC(C4=CC=CC=C4)=C3C)=C(C=C2CN5CCCCC5C(NCCN)=O)Cl)=C1.Cl.Cl
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PD-1/PD-L1-IN-63 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PD-1/PD-L1-IN-632691796-92-4PD-1/PD-L1CXCRPD-1/Programmed death-ligand 1CXC chemokine receptorsC-X-C motif chemokine receptorsH1299 cellscancer cell deathJurkat cellsPD-1/PD-L1 interactionimmune checkpoint humanized mouse modelsHeLa cellsHepG2 cellsMCF-7 cellstumor growthmelanomaInhibitorinhibitorinhibit

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