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Antitumor agent-169

Antitumor agent-169 (Compound B3) is a dual inhibitor PD-1/PD-L1 interaction and PARP7, with IC50s of 0.426 μM and 2.50 nM. Antitumor agent-169 exhibits an affinity to human PD-L1, with Ki of 20.2 nM. Antitumor agent-169 restores the T cell function, increases IFN-γ secretion. Antitumor agent-169 inhibits cell viability of MDA-MB-231 and Jurkat T, exhibits antitumor efficacy against melanoma in mouse model and good pharmacokinetic characteristics[1].

Product Specifications

CAS Number

[9007-83-4]

UNSPSC

12352005

Target

PARP; PD-1/PD-L1

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; Immunology/Inflammation

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/antitumor-agent-169.html

Smiles

CC1=C(C=CC=C1C2=CC=CC=C2)COC3=CC(OC)=C(C(OC)=C3)CN4CCCC[C@H]4C(NCCOCCOCCNC(C5=CN=C(N=C5)N6CCN(CC6)C(CCOC[C@@H](NC7=C(C(NN=C7)=O)C(F)(F)F)C)=O)=O)=O

Molecular Formula

C55H69F3N10O10

Molecular Weight

1087.19

References & Citations

[1]Gao Y, et al., Novel Bifunctional Conjugates Targeting PD-L1/PARP7 as Dual Immunotherapy for Potential Cancer Treatment. J Med Chem. 2024 Jun 24.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

PARP7

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