Drug intelligence / Profile preview

ALW-II-41-27

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraperitoneal, Likely Oral (noted Limitations In Preclinical Studies), Not Approved/established In Humans
01

Overview

ALW-II-41-27 is a **small molecule inhibitor** that selectively targets **EPH family receptor tyrosine kinases**, primarily **EPHA2**. It exhibits nanomolar potency with an IC50 of approximately 11 nM for EPHA2. ALW-II-41-27’s mechanism involves the inhibition of EPHA2-mediated signaling, affecting downstream pathways such as PI3K/AKT/mTOR, RAS/RAF/MAPK, FAK, SRC, ABL, and RHO/RAC/CDC42. Preclinically, it has demonstrated anti-tumor effects, reducing tumor growth and increasing apoptosis in non–small cell lung cancer (NSCLC) models. In vitro and in vivo studies indicate anti-inflammatory activity, particularly by suppressing proinflammatory cytokine release in models of *Pneumocystis* pneumonia and reducing atherosclerosis-related inflammation. The drug has also shown efficacy in suppressing cell survival, proliferation, migration, and invasion in various cancers, such as lung, cervical, breast, and nasopharyngeal cancers, through inhibition of EPHA2-dependent signaling (including via the RhoA/ROCK pathway and Shp2/Erk-1/2). ALW-II-41-27 is used in preclinical research and is not approved for clinical use.

02

Targets

Fgr proto-oncogene tyrosine-protein kinaseCSF1R (Macrophage colony-stimulating factor receptor)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)EPHA2 (Ephrin type-A receptor 2)EPHB2 (Ephrin type-B receptor 2)EPHA3 (Ephrin Receptor A3)LYN (LYN proto-oncogene, Src family tyrosine kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)FGFR3 (Fibroblast growth factor receptor 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)BMX (Bone Marrow Tyrosine Kinase X-linked)

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