2222689-47-4
Chemical Structure
Enrupatinib
Synonym(s): EI‐1071
- CAS No.: 2222689-47-4
- Formula:C27H26N6O3
- Molecular Weight:482.53
InChIKey: UGKFKFGVNJJPOL-UHFFFAOYSA-N
SMILES: N#CC1=C2N=C(N3CCOCC3)C=NC2=CC=C1NC4=CC=C(C(OC)=C4)OCC5=CN=C(C)C=C5
Biological Activity: Enrupatinib (EI‐1071) is a potent, orally active, CNS-penetrant and selective CSF1R inhibitor. Enrupatinib inhibits macrophage proliferation and osteoclast differentiation in vitro. Enrupatinib preserves microglia distal to Aβ plaques. Enrupatinib mitigates Alzheimer's disease (AD)-related pathologies by reducing neuroinflammation, preserving neuronal integrity, lowering disease-associated microglia gene expression, and enhancing cognitive function in 5xFAD and J20 mouse models. Enrupatinib reduces tumor-associated macrophage infiltration and enhances antitumor activity of anti-PD-1 antibody in murine colorectal cancer and breast cancer models. Enrupatinib can be used for the research of AD, colorectal cancer, and breast cancer[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Enrupatinib | 98.90% | Enrupatinib (EI‐1071) is a potent, orally active, CNS-penetrant and selective CSF1R inhibitor. Enrupatinib inhibits macrophage proliferation and osteoclast differentiation in vitro. Enrupatinib preserves microglia distal to Aβ plaques. Enrupatinib mitigates Alzheimer's disease (AD)-related pathologies by reducing neuroinflammation, preserving neuronal integrity, lowering disease-associated microglia gene expression, and enhancing cognitive function in 5xFAD and J20 mouse models. Enrupatinib reduces tumor-associated macrophage infiltration and enhances antitumor activity of anti-PD-1 antibody in murine colorectal cancer and breast cancer models. Enrupatinib can be used for the research of AD, colorectal cancer, and breast cancer. | ||||||||||||||||||||
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- [1]. Wahyu Dewi Tamayanti, et al. Significance of Enrupatinib, a CSF1R inhibitor, on Decreasing Neuroinflammation and Maintaining Neuronal Health in Mice Models of Alzheimer's Disease. Alzheimer's & DementiaVolume 21, Issue S5 e102542.
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[2]. Hung-Kai Chen, et al. Abstract 343_ A potent and selective cfms inhibitor EI-1071 inhibits CSF1R signaling and regulates the tumor-associated macrophages. Cancer Res
(2019) 79 (13_Supplement): 343.
Keywords