FGFR Inhibitor

ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC₅₀s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.

Lenvatinib (Standard) is the analytical standard of Lenvatinib. This product is intended for research and analytical applications. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.

Futibatinib (Standard) is the analytical standard of Futibatinib. This product is intended for research and analytical applications. Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC₅₀s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC₅₀s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM).

TYRA-200 is a potent and orally active FGFR2 inhibitor. TYRA-200 inhibits the kinase activity of wild-type FGFR2 and its mutants. TYRA-200 induces significant tumor regression in FGFR2-driven cancer models. TYRA-200 can be used for the research of FGFR2-altered advanced solid tumors, intrahepatic cholangiocarcinoma, and endometrial cancer.

IMC-D11 (LY-3076226 antibody) is an anti-FGFR3 IgG1 monoclonal antibody with an EC₅₀ of approximately 0.1 nM against hFGFR3b and hFGFR3c. IMC-D11 inhibits the growth of FGFR3-dependent lung adenocarcinoma in mouse models and shows no effect on tumors that do not express FGFR3. IMC-D11 can serve as an ADC Antibody for ADC synthesis, such as LY3076226. IMC-D11 is applicable to research related to urothelial carcinoma, multiple myeloma, lung adenocarcinoma, as well as advanced or metastatic cancers.

Lenvatinib-d₄ is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.

FGFR1 Human Pre-designed siRNA Set A contains three designed siRNAs for FGFR1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Infigratinib-Boc is a derivative of Infigratinib containing a Boc (t-Butyloxy carbonyl) group. Infigratinib is an ATP-competitive pan-FGFR inhibitor.

(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC₅₀s of 2.1, 0.008, and 1.2 µM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors.

FGFR4-IN-5 is a potent and selective covalent FGFR4 inhibitor with an IC₅₀ of 6.5 nM. FGFR4-IN-5 exhibits strong anti-tumor activity in vivo and can be used for hepatocellular carcinoma research.

SNIPER(TACC3)-11 is a potent FGFR3-TACC3 degrader. SNIPER(TACC3)-11 reduces FGFR3-TACC3 protein levels and suppressed the growth of FGFR3-TACC3 positive cancer cells.

CYY292 is an FGFR1 inhibitor that specifically targets the FGFR1/AKT/Snail pathway in GBM cells. CYY292 dose-dependently inhibits cancer cell proliferation, epithelial-mesenchymal transition, stemness, invasion, and migration in vitro.

KG-655 is a ligand that specifically binds to the ARNT PAS-B domain. KG-655 binds to the internal cavity of ARNT PAS-B to restrict its variable folded conformation, disrupts the interaction between ARNT PAS-B and the transcriptional coactivator TACC3, and promotes the homodimerization of ARNT PAS-B. KG-655 is widely applicable to cancer-related research.

FGFR2-IN-3 is an inhibitor of fibroblast growth factor receptor 2 (FGFR2). FGFR2-IN-3 has good binding properties, forming key interactions and inducing conformational changes in FGFR2. FGFR2-IN-3 can be used for research on tumors.

JK-P3 is a potent and pan VEGFR2 inhibitor, with IC₅₀s of 7.83 μM, 27 μM and 5.18 μM for VEGFR2, FGFR1 and FGFR3, respectively. JK-P3 can inhibit VEGF-A-stimulated VEGFR2 activation and intracellular signalling, also inhibits endothelial monolayer wound closure and angiogenesis, as well as fibroblast growth factor receptor kinase activity in vitro. JK-P3 has anti-angiogenic activity.

FGFR3 Human Pre-designed siRNA Set A contains three designed siRNAs for FGFR3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

TL13-68 is a biotin-tagged version of SM1-71, and it can be used to research the mechanism of SM1-71.

Lucitanib (E-3810) dihydrochloride is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC₅₀s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.

S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC₅₀ values below 20 nM.

R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with K_d values of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC₅₀ of 10 nM and 28 nM, respectively. R1530 triggers apoptosis (mitotic catastrophe) or senescence.