1. Immunology/Inflammation
  2. PD-1/PD-L1
  3. D5B

D5B is a potent and selective PD-L1 inhibitor. D5B has been modified by DBCO. The EC50 of D5B degrading PD-L1 in 4T1 and B16-F10 tumor cells are 5.4 μM and 6.2 μM, respectively. D5B can block PD-L1/PD-1 interaction and has anti-tumor activity.

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D5B

D5B Chemical Structure

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Description

D5B is a potent and selective PD-L1 inhibitor. D5B has been modified by DBCO. The EC50 of D5B degrading PD-L1 in 4T1 and B16-F10 tumor cells are 5.4 μM and 6.2 μM, respectively. D5B can block PD-L1/PD-1 interaction and has anti-tumor activity[1].

IC50 & Target

EC50: 5.4 μM (PD-L1 in 4T1 tumor cells)[1]
EC50: 6.2 μM (PD-L1 in B16-F10 tumor cells)[1]

In Vitro

D5B (0-10 μM; 24 h) can degrade PD-L1 in 4T1 and B16-F10 tumor cells with EC50 of 5.4 μM and 6.2 μM, respectively[1].
D5B (0-5 μM; 48 h) significantly decreases the PD-L1 abundance on cell membrane surface in IFN-γ treated and azide-labeled 4T1 and B16-F10 tumor cells[1].

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

Western Blot Analysis[1]

Cell Line: IFN-γ treated and azide-labeled 4T1 and B16-F10 tumor cells
Concentration: 0, 1.25, 2.5 and 5.0 μM
Incubation Time: 48 h
Result: Significantly reduced the level of PD-L1.
In Vivo

D5B (5 mg/kg; intravenous injection; single dose) has anti-tumor effects in mouse tumor models and is more effective in combination with radiotherapy. (D5B is in the form of PCPGd@D5B nanoparticles)[1]

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

Animal Model: 4T1 tumor-bearing mice with radiotherapy[1]
Dosage: 5 mg/kg (D5B is in the form of PCPGd@D5B nanoparticles)
Administration: Intraperitoneal injection (i.p.); Single dose
Result: Completely eradicated 50% of the tumor xenografts, with 60% of the tumor-bearing mice survived over 100 days.
Increased the percentage of tumor-infiltrating IFN-γ+CD8+ T cells.
Efficiently provoked an adaptive antitumor immune response for tumor regression.
Animal Model: B16-F10 tumor-bearing mice with radiotherapy[1]
Dosage: 5 mg/kg (D5B is in the form of PCPGd@D5B nanoparticles)
Administration: Intraperitoneal injection (i.p.); Single dose
Result: Suppressed 95% of tumor growth, with complete tumor elimination in 43% of the tumor-bearing mice and elongated survival time over 50 days.
Effectively suppressed PD-L1 expression on the surface of tumor cells and TAM membrane.
Promoted the increase of tumor infiltrating CD8+ T cells.
Molecular Weight

983.15

Formula

C58H66N2O12

SMILES

O=C(CCC(N1CC2=CC=CC=C2C#CC3=C1C=CC=C3)=O)OCCOCCOCCOCCOCCOC(C4N(CC5=C(OC)C=C(OCC6=CC=CC(C7=CC=CC=C7)=C6C)C=C5OC)CCCC4)=O

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • 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.

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Product Name:
D5B
Cat. No.:
HY-169392
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