Tag: Axl

XL092 is a Potent Axl, Mer and C-Met kinase Inhibitor

Human Axl belongs to the TAM subfamily of receptor tyrosine kinases that includes Mer. TAM kinases contain two immunoglobulin-like domains and two fibronectin type III domains. Many cancer cells exhibit overexpressed Axl. And it is initially cloned from patients with chronic myelogenous leukemia. Axl has been associated with cancers...

Cabozantinib is a potent Multiple Receptor Tyrosine Kinases (RTKs) Inhibitor

Receptor tyrosine kinases (RTKs) are high-affinity cell surface receptors for many polypeptide growth factors, cytokines, and hormones. Specifically, RTKs are part of a larger family of protein tyrosine kinases. RTKs are key regulators of normal cellular processes. Besides, it plays a key role in the development and progression of...

ONO-7475 is a Selective and Orally Active AXL/Mer Inhibitor

EGFR tyrosine kinase inhibitors (EGFR-TKIs) are efficient for the treatment of non-small cell lung cancer (NSCLC) harboring EGFR mutations. However, most EGFR-positive NSCLC patients exhibit resistance to EGFR-TKIs after sometimes. The 3rd generation EGFR-TKI Osimertinib shows efficacy for overcoming EGFR T790M mutation-positive NSCLC. Anexelekto (AXL) belongs to the TAM...

BPI-9016M is an Orally Active and Selective Dual c-Met/AXL Inhibitor

c-Met is a membrane-spanning receptor tyrosine kinase. It has a high affinity for binding to hepatocyte growth factor (HGF). As we all know, HGF/c-Met signaling often involves activation of its downstream pathways. High-level Met gene amplification, mutation or protein overexpression can lead to aberrant activation of the HGF/c-Met pathway. In...

RU-302, a pan-TAM Inhibitor, Blocks Gas6-Inducible TAM Activation and Tumorigenicity

The TAM receptors (Tyro-3, Axl, and Mertk) are a family of three homologous types I receptor tyrosine kinases (RTKs). They play an indispensable role in homeostasis and the resolution of inflammation under physiological conditions. Pathophysiologically, TAMs frequently overexpressed in a wide variety of human cancers that are associated with...