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CXF-009 is a potent, specific, dual-warhead covalent inhibitor of FGFR4 (IC50=48 nM), forms dual-warhead covalent bonds with two cysteine residues in FGFR4.CXF-009 forms covalent bonds with FGFR4(C477A) and FGFR4(C552A), respectively; display weak inhibition against FGFR1-3 with IC50 of 2579 nM, 2408 nM, and 977 nM.CXF-009 shows inhibitory effect agaginst FGFR4 muntants FGFR4(C477A), FGFR4(C552A), and FGFR4(C477A, C552A) with IC50 of 193 nM, 602 nM, and 1528 nM, respectively.CXF-009 inhibited the growth of Ba/F3 cells transformed with FGFR1-4 with IC50 values of 1562 nM, 1971 nM, 777 nM, and 38 nM, respectively.CXF-009 is slightly more reactive to GSH than PRN1371.
FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM and 3.2 nM, respectively. Antitumor activity.
Derazantinib (Derazantinib) is an ATP competitive tyrosine kinase inhibitor; exhibits potent activity against FGFR1-3 chondrocytes with IC50s of 4.5, 1.8, and 4.5 nM, respectively.
Siphonaxanthin is a keto-carotenoid with anti-angiogenic and anti-inflammatory activity, which is found in green algae. Siphonaxanthin upregulates the expression of death receptor 5 (DR5), induces cancer cell apoptosis, decreases the expression of Bcl-2, and activates caspase-3. Siphonaxanthin is also an inhibitor of FGFR-1. Siphonaxanthin inhibits the proliferation, migration, and tube formation of human umbilical vein endothelial cells (HUVECs), as well as the outgrowth of microvessels in the rat aortic ring. Siphonaxanthin is promising for research of diseases such as cancer, diabetic retinopathy, and rheumatoid arthritis.
PNU-145156E (FCE26644) is an angiogenesis inhibitor with anti-tumor activity. PNU-145156E inhibits the binding of bFGF to its receptor and inhibits bFGF-induced endothelial cell proliferation and motility.
BW710 is an orally active fibroblast growth factor receptor 2 (FGFR2) inhibitor. BW710 inhibits the proliferation of BaF3-FGFR2 cells with an IC50 of 2.8 nM. BW710 abolishes FGFR2 enzymatic activity and is selective against other 75 tyrosine kinases including FGFR1, FGFR3, and FGFR4 at 1 μM. BW710 suppresses the FGFR2 signaling and selectively inhibits FGFR2-driven cancer cell proliferation. BW710 displays reasonable
pharmacokinetic properties with an oral bioavailability of 29 % in mice.