SPH5030 is a Selective and Irreversible HER2 Inhibitor.
HER2 is a member of the human epidermal growth factor receptor (HER/EGFR/ERBB) family. Importantly, HER2 plays a crucial role in the regulation of cell growth, differentiation, and survival. Specifically, HER2 is the only member in the HER family without a specific ligand, so its overexpression accordingly can lead to...
BI-1622 is an Orally active and Selective HER2 Inhibitor
BI-1622 is an orally active, potent, and highly selective HER2 (ERBB2) inhibitor, with IC50 values of 7.8, 7.1, <5.3 nM for HER2WT, HER2YVMA, EGFRWT, respectively. Besides, BI-1622 shows greater than 25-fold selectivity over EGFR. Moreover, BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models. HER2 is a member...
HS-131 is a near Infrared Dye Tethered Hsp90 Inhibitor
Hsp90 (heat shock protein 90) is a molecular chaperone protein. Specifically, Hsp90 can help other proteins fold correctly, stabilize proteins, resist heat stress, and contribute to protein degradation. It can also stabilize many proteins needed for tumor growth. Besides, Hsp90 is present in all branches of bacteria and eukaryotes....
Aderbasib is a Highly Potent and Orally Active Inhibitor of ADAM10 and ADAM17
ADAMs (a disintegrin and metalloproteinases), originally also known as MDC proteins (metalloproteinase/disintegrin/cysteine-rich). And ADAMs belong to the Metzincins superfamily of metalloproteases. Recently, studies have found ADAM genes exist in animals, choanoflagellates, fungi and some groups of green algae. Importantly, ADAMs mediates proteolytic ectodomain release. And the ectodomain shedding is...
BDTX-189 is an Orally Active Inhibitor of Allosteric EGFR and HER2 Oncogenic Mutations
Epidermal growth factor receptor (EGFR) is a growth-factor-receptor tyrosine kinase. Elevated levels of the EGFR, and/or its cognate ligands act as a common component of multiple cancer types and appear to promote solid tumor growth. BDTX-189 is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations....
AZD-9833 is an Orally Active Estrogen Receptor (ER) Antagonist
Estrogens participate in numerous physiological processes such as cell growth, reproduction, and differentiation. In females, the ovaries are the major site of estrogen synthesis producing the predominant estrogen 17b-estradiol (E2). In addition to effects by E2 on normal physiology, estrogens also play an important role in several pathological processes...