FGFR

FGFR1/DDR2 inhibitor 1 is an inhibitor of discoidin domain receptor 2 (DDR2) and fibroblast growth factor receptor 1 (FGFR1), with IC50 values of 31.1 nM, 108.4 nM, and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.

FGFR4-IN-1 is a potent FGFR4 inhibitor (IC50: 0.7 nM).

Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity. Lenvatinib has the strongest inhibitory activity on VEGFR2 and VEGFR3 (IC50=4/5.2 nM). Lenvatinib has strong anti-tumor activity.

Nintedanib (Intedanib) is a triple vascular kinase inhibitor that inhibits VEGFR1, VEGFR2, and VEGFR3 (IC50=34 13 13 nM), FGFR1, FGFR2, and FGFR3 (IC50=69 37 108 nM), PDGFRα, and PDGFRβ (IC50=59 65 nM). Nintedanib has antitumor activity and inhibits tumor growth by inhibiting angiogenesis.

CP-547632 is an orally available and potent, ATP-competitive dual inhibitor of VEGFR-2 and FGF kinase F with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective, with higher selectivity for VEGFR2 and bFGF than for EGFR, PDGFRβ and related tyrosine kinases (TKs). PDGFRβ and related tyrosine kinases (TKs) CP-547632 has antitumour activity.

TG 100572 Hydrochloride is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively).

FIIN-4 is a covalent inhibitor of FGFR and can be used in studies about metastatic breast cancer.

Pazopanib (GW786034) is an inhibitor of protein tyrosine kinases that inhibits VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms (IC50=10 30 47 84 74 140 146 nM). Pazopanib has antitumor activity.

Formononetin (Flavosil) is an O-methylated isoflavone and a phytoestrogen from the root of Astragalus membranaceus.

Regorafenib (BAY 73-4506) is an orally active, multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ, exhibiting both antitumor and anti-angiogenic activity.

Ferulic Acid (Coniferic acid) is a highly abundant phenolic phytochemical and a type of organic compound found in the Ferula assafoetida L. or Ligusticum chuanxiong.It can be absorbed by the small intestine and excreted through the urine.

Ponatinib (AP24534) is an orally available, multitargeted kinase inhibitor with IC50 values of 0.37 nM (Abl), 1.1 nM (PDGFRα), 1.5 nM (VEGFR2), 2.2 nM (FGFR1), and 5.4 nM (Src).

2,5-Dihydroxybenzoic acid (Gentisic acid) is an active metabolite of salicylic acid degradation with a broad spectrum of biological activity, such as anti-inflammatory, antirheumatic and antioxidant properties.

Erdafitinib (JNJ-42756493), a quinoxaline derivative, targets FGFR1/2/3/4.

Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor targeting VEGFR1/2/3, FGFR1/2/3, and PDGFRα/β.

Pazopanib Hydrochloride (Votrient HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.

Lenvatinib mesylate (E7080 (mesylate)) is an oral and multi-targeted inhibitor of VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, with potent antitumor activities.

Roblitinib (FGF-401) is an inhibitor of human fibroblast growth factor receptor 4 (FGFR4) with potential antineoplastic activity. Upon administration, Roblitinib binds to and inhibits FGFR4, leading to the inhibition of tumor cell proliferation in FGFR4-overexpressing cells. It is a receptor tyrosine kinase upregulated in certain tumor cells and involved in proliferation, differentiation, angiogenesis, and survival.

PP58 is an inhibitor of PDGFR, FGFR and Src family.

JK-P3 is a pyrazole-based inhibitor of VEGFR-2 (IC50: 7.8 μM). JK-P3 inhibits FGFR 1 3 kinase activity in vitro, but has no effect on FGFR signaling in cell-based assays. The compound blocks wound healing and tube formation in HUVEC without effecting endo

Pemigatinib (INCB054828) is an orally active, selective inhibitor of FGFR, with IC50 values of 0.4 nM for FGFR1, 0.5 nM for FGFR2, 1.2 nM for FGFR3, and 30 nM for FGFR4.

Rogaratinib (BAY1163877) is an aberrant inhibitor of fibroblast growth factor receptor (FGFR). Rogaratinib is as an orally available, selective and potent inhibitor of FGFR-1, -2 and -3 kinase activity.

SKLB610, a novel multi-targeted inhibitor, inhibits angiogenesis-related tyrosine kinase VEGFR2, FGFR2, and PDGFR at a rate of 97%, 65%, and 55%, respectively, at the concentration of 10 μM in biochemical kinase assays.

Heparan sulfate is a natural product, a linear polysaccharide. Heparan sulfate occurs as a proteoglycan (HSPG) that is tightly attached to cell surface or extracellular matrix proteins.