Category: Lung Adenocarcinoma

BM-1197 is a Potent and Selective Dual Bcl-2/Bcl-xL Inhibitor

Bcl-2 and Bcl-xL are critical regulators of apoptosis. The pharmacological inhibition of Bcl-2 and Bcl-xL represents a promising strategy for cancer treatment. In addition, BM-1197 is a potent and efficacious dual inhibitor of Bcl-2 and Bcl-xL. BM-1197 binds to Bcl-2 and Bcl-xL proteins with Ki values less than 1...

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...

MRTX849 is an Orally Active and Covalent Inhibitor of KRAS G12C

KRAS mutations are the most common mutations. Especially, the KRAS oncogene encodes a binding protein that plays a crucial role in transmitting signals from extracellular growth factors to the cell nucleus. KRAS mutations occur commonly in colorectal carcinomas. KRASG12C mutations are present in lung and colon adenocarcinoma as well...

Tasisulam, an Antitumor Agent, Inhibits Mitotic Progression and Induces Apoptosis

Tasisulam is an acyl sulfonamide with a unique antitumor dual mechanism of action. It involves antiangiogenesis and mitotic inhibition. Tasisulam has a broad range of activity in 60 tumor cell lines. It includes leukemia, melanoma, non-small-cell lung cancer, colon, ovarian, renal, and breast cancers. In this study, Tasisulam is...

EC0489, a SMDC for Cancer Therapy

Small molecule drug conjugates (SMDCs) contain three parts: a targeting ligand, a linker and a drug payload. SMDCs have their own strengths such as manageable synthesis and a non-immunogenic nature. The molecular weights of SMDCs are potentially much lower, and lead to good cell penetration in tumors and better...