1. Immunology/Inflammation
    Apoptosis
  2. PD-1/PD-L1
    Apoptosis
  3. PD-1/PD-L1-IN-10

PD-1/PD-L1-IN-10 

Cat. No.: HY-132202
Handling Instructions

PD-1/PD-L1-IN-10 (compound B2) is an orally active PD-1/PD-L1 inhibitor (IC50 of 2.7 nM) with potent anticancer efficacy.

For research use only. We do not sell to patients.

PD-1/PD-L1-IN-10 Chemical Structure

PD-1/PD-L1-IN-10 Chemical Structure

CAS No. : 2487550-41-2

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Description

PD-1/PD-L1-IN-10 (compound B2) is an orally active PD-1/PD-L1 inhibitor (IC50 of 2.7 nM) with potent anticancer efficacy[1].

IC50 & Target

IC50: 2.7 nM (PD-1/PD-L1)[1].

In Vitro

PD-1/PD-L1-IN-10 (compound B2) significantly promotes interferongamma secretion in a dose-dependent manner in vitro even at the low concentration of 1 nM[1].
PD-1/PD-L1-IN-10 (compound B2) does not affect cell viability of LLC cells and lymph node T-cells[1].
PD-1/PD-L1-IN-10 (compound B2, 0-100 nM) stabilizes the PD-L1 protein in mouse Lewis lung carcinoma (LLC) cells. In particular, PD-1/PD-L1-IN-10 (compound B2) maintains the PD-L1 stability in a dose-dependent manner at 58 °C. Suggesting that PD-1/PD-L1-IN-10 (compound B2) could enter LLC cells and then directly binds to the PD-L1 protein[1].

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

In Vivo

PD-1/PD-L1-IN-10 (compound B2, 5 mg/kg, intragastric gavage) exhibits potent in vivo anticancer efficacy in an LLC-bearing allograft mouse model. PD-1/PD-L1-IN-10 (compound B2) effectively blocks tumor cell proliferation and induces apoptosis in LLC tumor tissues.[1].

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

Animal Model: LLC tumor-bearing mice[1].
Dosage: 2, 5 mg/kg.
Administration: i.g., qd., for 21 days
Result: Significantly suppressed the growth of the tumor in a dose-dependent manner compared with the vehicle group.
Molecular Weight

581.62

Formula

C₃₃H₃₁N₃O₇

CAS No.
SMILES

CC1=C(C=CC=C1C2=CC=CC=C2)COC3=C(C=C(C(OCC4=CC(C#N)=CC=C4)=C3)CN[[email protected]](C(O)=O)C(O)C)[N+]([O-])=O

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

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Keywords:

PD-1/PD-L1-IN-10PD-1/PD-L1ApoptosisPD-1/Programmed death-ligand 1LewislungcarcinomaLLCtumorT-lymphocyteIFN-γ,Inhibitorinhibitorinhibit

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PD-1/PD-L1-IN-10
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