1. Immunology/Inflammation
  2. PD-1/PD-L1
  3. PD-L1-IN-5

PD-L1-IN-5 (X22) is an orally active PD-L1 inhibitor, with the IC50 value of 785.6 nM. PD-L1-IN-5 has anti-tumor activity in vivo.

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PD-L1-IN-5 Chemical Structure

PD-L1-IN-5 Chemical Structure

CAS No. : 2597056-85-2

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Description

PD-L1-IN-5 (X22) is an orally active PD-L1 inhibitor, with the IC50 value of 785.6 nM. PD-L1-IN-5 has anti-tumor activity in vivo[1].

In Vitro

PD-L1-IN-5 (X22) (0-150 μM, 12 h) has no obvious cytotoxic effect on MC38 and CT26 cells in vitro[1].

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

In Vivo

PD-L1-IN-5 (X22) (0-50 mg/kg/day for 20 days, p.o.) demonstrates significant antitumor efficacy in murine models of MC38 and CT26 colon cancer through the upregulation of tumor infiltration and cytotoxicity of CD8 + T cells partially, but exhibits low antitumor effect in the syngeneic CT26 colorectal cancer model in immunodeficient nude mice which indicated that the antitumor mechanism relies on the immune system [1].

Pharmacokinetic Analysis in SD rats and C57blo/6 mice[1]

Animal model Route Dose (mg/kg) t1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng·h/mL) CL (mL/h/kg) F (%)
SD rat p.o. 45 4.3 4.00 49.8 405.6 / 3.4
C57blo/6 mice p.o. 10 1.6 0.7 255.7 315.6 / 11.5

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

Animal Model: MC38 and CT26 tumor mouse model, Balb/c mice (female, 8 week old)[1]
Dosage: 0-50 mg/kg/day for 20 days
Administration: p.o.
Result: Inhibited colon tumor growth in mice with tumor growth inhibition rates (TGI) of 49.5% and 73.6% at doses of 5 mg/kg and 25 mg/kg, respectively.
Molecular Weight

763.25

Formula

C40H44ClFN4O8

CAS No.
SMILES

OC1CCN(CCCOC2=CC=CC(C3=CC=CC(COC4=C(Cl)C=C(CN[C@@H](C(OCC)=O)CO)C(OCC5=CC6=NON=C6C=C5)=C4)=C3F)=C2)CC1

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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-L1-IN-5 Related Classifications

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    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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PD-L1-IN-5
Cat. No.:
HY-162357
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