FGFR1 Inhibitor

Risimtinib (Risimtinibum) is a FGFR1 inhibitor with an IC₅₀ of 2.1 nM. Risimtinib inhibits the proliferation of FGFR1-positive cancer cells. Risimtinib is used for the research of myeloid leukemia.

SU10944 is a selective, orally active VEGFR inhibitor, with an IC₅₀ of 6 nM against VEGFR-1, an IC₅₀ of 96 nM and a K_i of 21 nM against VEGFR-2. SU10944 only exhibits weak inhibitory activity against PDGFRβ (IC₅₀ = 1 μM), SCFR (IC₅₀ = 1.58 μM) and FGFR-1 (IC₅₀ = 1.6 μM). SU10944 selectively inhibits VEGFR receptor downstream signaling, neovascularization, vascular permeability, VEGF-mediated tissue factor production, and induces tumor growth delay. SU10944 can be used in research related to diabetic retinopathy, exudative age-related macular degeneration or cancer.

FGFR-IN-27 is an orally active, broad-spectrum FGFR inhibitor, with an IC₅₀ of 0.24 nM against human FGFR1, 0.71 nM against FGFR2, 0.87 nM against FGFR3, and 6.50 nM against FGFR4. FGFR-IN-27 inhibits cancer cell proliferation and blocks tumor growth. FGFR-IN-27 reduces the phosphorylation levels of AKT and ERK, induces apoptosis and ferroptosis, increases ROS levels, and decreases GSH levels. FGFR-IN-27 can be used in the research of hepatocellular carcinoma.

FGFR-IN-28 is a FGFR inhibitor with inhibitory activity against multiple subtypes of the FGFR family, with an IC₅₀ of 4.4 nM against FGFR4. FGFR-IN-28 inhibits kinase activity and phosphorylation processes, and blocks the downstream MAPK and AKT signaling pathways. FGFR-IN-28 induces cellular DNA damage, cell cycle arrest, apoptosis and ferroptosis, and reduces the adhesion, invasion and metastasis abilities of cancer cells. FGFR-IN-28 exhibits anti-tumor activity in in vitro experiments on colon cancer cells, and inhibits tumor growth in colon cancer xenograft models. FGFR-IN-28 can be used in colon cancer-related research.

PD173074 GMP is PD173074 (HY-10321) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. PD173074 is an orally active FGFR inhibitor that targets the transphosphorylation of FGFR1 and FGFR2 and blocks the FGF signaling pathway. By reducing the phosphorylation level of SMAD2 and altering the expression of Nodal/Activin target genes, PD173074 eliminates endothelial differentiation potential, thereby inhibiting the formation of capillary-like structures. PD173074 blocks the proliferation and colony formation of tumor cells and increases intratumoral cell apoptosis. PD173074 successfully reverses FGF-2-induced chemoresistance to enhance the effect of cisplatin (HY-17394) in small cell lung cancer models. PD173074 can be applied to research related to critical limb ischemia and small cell lung cancer.

FGFR3-IN-12 is a selective fibroblast growth factor receptor 3 (FGFR3) inhibitor with an IC₅₀ of 6.8 nM. FGFR3-IN-12 shows an IC₅₀ of 19.2 nM against FGFR3^V555M and an IC₅₀ of 16.9 nM against TNK1 (Thirty-eight Negative Kinase 1). FGFR3-IN-12 inhibits cancer cells proliferation and induces caspase-mediated apoptosis. FGFR3-IN-12 exhibits antitumor activity in bladder cancer xenografts mice models. FGFR3-IN-12 can be used for the research of cancer, such as bladder cancer.

FGFR-IN-12 (example 14), a pyrimidinyl aryl urea derivative, is a potent FGFR inhibitor.

Anti-Mouse Delta-like protein 4/DLL4 Antibody (HMD4-2) is an anti-mouse Delta-like protein 4/DLL4 IgG monoclonal antibody. Anti-Mouse Delta-like protein 4/DLL4 Antibody (HMD4-2) can reduce angiogenesis and density by blocking the DLL4-Notch signaling pathway. Anti-Mouse Delta-like protein 4/DLL4 Antibody (HMD4-2) reduces inflammatory response by decreasing NF-κB activity and pro-inflammatory factors (IL-1β, iNOS, IL-6) levels. Anti-Mouse Delta-like protein 4/DLL4 Antibody (HMD4-2) can inhibit Th17 cell differentiation and IL-17A production. Anti-Mouse Delta-like protein 4/DLL4 Antibody (HMD4-2) can reduce macrophage infiltration and alleviate insulin resistance. Anti-Mouse Delta-like protein 4/DLL4 Antibody (HMD4-2) can be used for researches on inflammation, metabolic conditions and cancer such as atherosclerosis, pancreatic cancer and asthma.