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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