PD-1/PD-L1-IN-67
PD-1/PD-L1-IN-67 is a PD-L1/PD-L1 interaction inhibitor with an IC50 of 55.11 nM. PD-1/PD-L1-IN-67 directly blocks the PD-1/PD-L1 interaction and downregulates PD-L1 expression at both mRNA and protein levels. PD-1/PD-L1-IN-67 acts synergistically with radiotherapy to inhibit cancer cell viability, clonogenic survival, migration and invasion, and induce apoptosis. PD-1/PD-L1-IN-67 can be used in the research of non-small cell lung cancer.
For research use only. We do not sell to patients.
- Formula: C25H29N3O4
- Molecular Weight:435.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
PD-1/PD-L1-IN-67 (Compound N02) (24-72 h) exerts selective dose- and time-dependent cytotoxicity against HCC78 and H2122 non-small cell lung cancer (NSCLC) cells, with IC50 values as low as 4.57 μM (HCC78, 72 h) and 3.72 μM (H2122, 72 h); it produces additive cytotoxic effects when combined with X-ray irradiation[1].
PD-1/PD-L1-IN-67 (4-5 μM; 24 h) inhibits the clonogenic survival of HCC78 and H2122 non-small cell lung cancer (NSCLC) cells, with the strongest efficacy when combined with X-ray irradiation[1].
PD-1/PD-L1-IN-67 (4-5 μM) downregulates PD-L1 mRNA expression in HCC78 and H2122 non-small cell lung cancer (NSCLC) cells, with the strongest effect when combined with X-ray irradiation[1].
PD-1/PD-L1-IN-67 (4-5 μM; 48 h) enhances the inhibitory effect of radiation on the migration of HCC78 and H2122 non-small cell lung cancer (NSCLC) cells, with the strongest efficacy when combined with X-ray irradiation[1].
PD-1/PD-L1-IN-67 (4-5 μM; 24 h) significantly enhances the inhibitory effect of radiation on the invasion of HCC78 and H2122 non-small cell lung cancer (NSCLC) cells, with the strongest efficacy when combined with X-ray irradiation[1].
PD-1/PD-L1-IN-67 (4-5 μM) enhances radiation-induced apoptosis of H2122 non-small cell lung cancer (NSCLC) cells, with the strongest effect when combined with X-ray irradiation[1].
PD-1/PD-L1-IN-67 (5 μM) downregulates the protein expression of PD-L1, Bcl-2 and Ki-67, and upregulates the expression of Caspase-3 in HCC78 non-small cell lung cancer cells; its effect is enhanced when used in combination with X-ray irradiation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human NSCLC HCC78 and H2122 cell lines
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Concentration:5 μM (HCC78 cells, alone); 4 μM (H2122 cells, alone); 5 μM (HCC78 cells, combined with 4 Gy irradiation); 4 μM (H2122 cells, combined with 6 Gy irradiation)
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Incubation Time:24 h
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Result:Reduced clonogenic capacity to 21.67% of control in H2122 cells when used alone.
Reduced clonogenic capacity to 6.09% of control in HCC78 cells and 9.10% of control in H2122 cells when combined with X-ray irradiation.
Showed a significant interaction with irradiation in HCC78 cells.
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Cell Line:human NSCLC HCC78 and H2122 cell lines
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Concentration:5 μM (HCC78 cells, combined with 4 Gy irradiation); 4 μM (H2122 cells, combined with 6 Gy irradiation)
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Incubation Time:48 h
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Result:Reduced migration rate to 17.91% of control in HCC78 cells when combined with X-ray irradiation.
Reduced migration to 26.42% of control in H2122 cells when combined with X-ray irradiation.
Showed a significant interaction with irradiation in H2122 cells.
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Cell Line:human NSCLC HCC78 and H2122 cell lines
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Concentration:5 μM (HCC78 cells, combined with 4 Gy irradiation); 4 μM (H2122 cells, combined with 6 Gy irradiation)
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Incubation Time:24 h
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Result:Reduced HCC78 cell invasion to 42.54% of control when combined with X-ray irradiation.
Reduced H2122 cell invasion to 25.82% of control when combined with X-ray irradiation.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (male, 4-6 weeks old)[1]
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Dosage:20 mg/kg (monotherapy); 20 mg/kg + 6 Gy focal tumor irradiation (combination)
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Administration:i.p.; every two days; 45 days
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Result:Produced a modest antitumor effect as monotherapy.
Resulted in significantly greater tumor growth suppression, substantially smaller final tumor volumes, and markedly lower final tumor weights compared to vehicle control, monotherapy, and radiation monotherapy when combined with focal tumor irradiation.
Significantly downregulated Ki-67 and PD-L1 protein expression, while upregulating Caspase-3 expression in tumor tissues when combined with focal tumor irradiation.
Reduced Ki-67 and PD-L1 protein expression to a lesser degree than the combination as monotherapy.
Chemical Information
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Molecular Weight 435.52
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Formula C25H29N3O4
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SMILES
COC1=NC(OCC2=C(C(C3=CC=C4OCCOC4=C3)=CC=C2)C)=CC=C1CNCCN
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PD-1/PD-L1-IN-67 Related Classifications
HY-187184 Related Classifications
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