Product Data Sheet

Enrupatinib

Catalog No. A34603

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Enrupatinib is a selective inhibitor of colony-stimulating factor 1 receptor (CSF1R) with potent oral bioavailability and central nervous system (CNS) penetration. It effectively inhibits macrophage proliferation and osteoclast differentiation in vitro, thereby mitigating neuroinflammation and preserving neuronal integrity in Alzheimer's disease models. Enrupatinib has demonstrated the ability to reduce disease-associated microglia gene expression and enhance cognitive function in 5xFAD and J20 mouse models. Additionally, it attenuates tumor-associated macrophage infiltration and improves the antitumor efficacy of anti-PD-1 antibodies in preclinical models of colorectal and breast cancer, making it a valuable tool for research in these areas.
Chemical Information
Catalog NumA34603
M. Wt482.53
FormulaC27H26N6O3
Purity>98%
Storageat -20 °C 3 years (powder form); at -20 °C 6 months (Solution base)
CAS No.2222689-47-4
SynonymsEI‐1071
SMILESN#CC1=C2N=C(N3CCOCC3)C=NC2=CC=C1NC4=CC=C(C(OC)=C4)OCC5=CN=C(C)C=C5
Biological Activity
DescriptionEnrupatinib is a selective inhibitor of colony-stimulating factor 1 receptor (CSF1R) with potent oral bioavailability and central nervous system (CNS) penetration. It effectively inhibits macrophage proliferation and osteoclast differentiation in vitro, thereby mitigating neuroinflammation and preserving neuronal integrity in Alzheimer's disease models. Enrupatinib has demonstrated the ability to reduce disease-associated microglia gene expression and enhance cognitive function in 5xFAD and J20 mouse models. Additionally, it attenuates tumor-associated macrophage infiltration and improves the antitumor efficacy of anti-PD-1 antibodies in preclinical models of colorectal and breast cancer, making it a valuable tool for research in these areas.
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