FGFR

AZ8010 is a selective inhibitor targeting fibroblast growth factor receptors 1 to 3 (FGFR1-3). It exhibits significant anti-proliferative activity, making it a valuable tool for cancer research. This compound can be utilized in studies exploring FGFR-related signaling pathways and their implications in tumorigenesis.

FGFR1 inhibitor-15 is a selective inhibitor of Fibroblast Growth Factor Receptor 1 (FGFR1), exhibiting an IC50 value of 27 μM. This compound is valuable for cancer research, facilitating the investigation of FGFR1 signaling pathways and their implications in tumor growth and development. Its use can contribute to the understanding of FGFR1-related oncogenic mechanisms and the potential for therapeutic targeting in malignancies.

FGFR1 Inhibitor-16 is a selective inhibitor of Fibroblast Growth Factor Receptor 1 (FGFR1). This compound demonstrates an inhibitory efficacy of 53.00% at a concentration of 50 μM and 24.95% at 10 μM. FGFR1 Inhibitor-16 is valuable for research applications focused on cancer, allowing for the exploration of FGFR1 signaling pathways and their roles in tumor biology.

FGFR1 inhibitor-17 is a potent inhibitor targeting fibroblast growth factor receptor 1 (FGFR1). This compound demonstrates significant anti-proliferative activity in various cancer models, making it a valuable tool for cancer research. Its ability to inhibit FGFR1 signaling pathways can aid in the investigation of tumor biology and the development of targeted therapies.

SSR128129E free acid is an allosteric inhibitor of fibroblast growth factor receptors (FGFR), exhibiting an IC50 of 1.9 μM for FGFR1. This compound demonstrates significant biological activity in modulating FGFR signaling pathways, making it valuable for research into cancer and other diseases associated with FGFR dysregulation. Its oral availability further facilitates in vivo studies and therapeutic exploration.

FGFR-IN-12 is a selective inhibitor of the Fibroblast Growth Factor Receptor (FGFR). This pyrimidinyl aryl urea derivative exhibits potent inhibition of FGFR activity, making it a valuable tool for investigating pathways involving FGFR signaling. Its efficacy positions FGFR-IN-12 as a significant compound for research applications related to cancer biology and therapeutic development targeting FGFR-related diseases.

Segigratinib hydrochloride is a selective inhibitor of FGFR1, FGFR2, FGFR3, and CSF-1R, exhibiting IC50 values of 0.5 nM, 1.3 nM, 3.6 nM, and 3.8 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its ability to target multiple receptors involved in tumor progression highlights its potential for therapeutic applications in oncology.

FGFR4-IN-7 is a covalent reversible inhibitor of Fibroblast Growth Factor Receptor 4 (FGFR4), exhibiting an IC50 of 0.42 μM. This compound disrupts the FGFR4 signaling pathway, leading to the induction of apoptosis. FGFR4-IN-7 is primarily utilized in research focused on hepatocellular carcinoma (HCC) and offers potential insights into therapeutic strategies targeting this malignancy.

HDAC-IN-50 is a potent dual inhibitor targeting FGFR and HDAC with IC50 values of 0.18 nM for FGFR1, 1.2 nM for FGFR2, 0.46 nM for FGFR3, 1.4 nM for FGFR4, and varying inhibitory effects on HDAC isoforms such as HDAC1 (1.3 nM), HDAC2 (1.6 nM), HDAC6 (2.6 nM), and HDAC8 (13 nM). This compound effectively induces apoptosis and causes cell cycle arrest at the G0/G1 phase. Additionally, HDAC-IN-50 decreases the expression of phosphorylated forms of FGFR1, ERK, and STAT3, indicating its potential applications in cancer research and therapy.

FGFR-IN-8 is a potent pan-FGFR inhibitor that targets both wild-type and mutant forms of fibroblast growth factor receptors (FGFRs). With impressive inhibitory potency, it demonstrates IC50 values of less than 0.5 nM against FGFR1, V564F-FGFR2, and FGFR3, alongside 22.6 nM for V555M-FGFR3, and 7.30 nM for FGFR4. This compound induces apoptosis in cancer cells and exhibits notable anticancer properties, making it a valuable reagent for cancer research and therapeutic studies involving FGFR signaling pathways.

Picrasidine Q is a FGFR2 kinase inhibitor derived from the alkaloid components of Angelica keiskei. It exhibits significant anti-cancer properties by inducing apoptosis and causing G1 phase cell cycle arrest in human esophageal cancer cell lines. This compound is valuable for research focused on cancer biology and the molecular mechanisms underlying cell transformation and proliferation.