fibroblast growth factor receptor

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.

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).

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.

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.

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).

Ferulic acid sodium (Sodium ferulic), the sodium salt of ferulic acid, is a drug used in traditional Chinese medicine for treatment of cardiovascular and cerebrovascular diseases and to prevent thrombosis.

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

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

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

SU4984 is a cell-permeable, ATP-competitive and reversible inhibitor of the fibroblast growth factor receptor 1 (FGFR1).

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.

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.

Lucitanib (E-3810) is a novel and potent inhibitor of VEGFR and FGFR, selectively targeting VEGFR1, VEGFR2, VEGFR3, FGFR1, and FGFR2 with IC₅₀ values of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.

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.

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.

AZD4547 is an FGFR family inhibitor. AZD4547 selectively inhibits FGFR1 phosphorylation and suppresses cancer cell proliferation through inhibition of FGFR1 signaling, and is able to act on FGFR1 (IC₅₀:0.2 nM), FGFR2 (IC₅₀:2.5 nM), FGFR3 (IC₅₀:1.8 nM) and FGFR4 (IC₅₀:165 nM). IC₅₀:165 nM).[2]

Infigratinib (NVP-BGJ398) (BGJ398) is an orally bioavailable pan FGFR inhibitor (IC₅₀: 0.9/1.4/1 nM for FGFR1/2/3), >40-fold selective for FGFR versus FGFR4 and VEGFR2.

PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC₅₀ of 39.9 nM and a Ki of 42 nM. It also inhibits the PDGFR, EGFR, and c-Src tyrosine kinases with IC₅₀ values of 310 nM, 240 nM, and 44 nM, respectively.

KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 (IC₅₀: 6.6 nM), modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-1R, EGFR.

BLU9931 is the first selective small molecule inhibitor of FGFR4.

ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα.