FGFR2-IN-1 is an FGFR inhibitor that inhibits FGFR1, FGFR2, and FGFR3 with IC50s of 460, 140, and 2200 nM, respectively.FGFR2-IN-1 can be used for the study of cancers associated with FGFR2.CAS 번호13460-73-81-1

FGFR2-IN-2 is a specific FGFR2 inhibitor that inhibits FGFR1, FGFR2, and FGFR3, and can be used in the study of cancer and cardiovascular disease.

FGFR2-IN-3 hydrochloride is a selective, orally active FGFR2 inhibitor.

FGFR2-IN-3 is an orally active selective FGFR2 inhibitor[1].

Aprutumab (BAY 1179470) is a human FGFR2 monoclonal antibody with affinity to FGFR2 isoforms FGFR2-IIIB and FGFR2-IIIC. Aprutumab is commonly used to synthesize antibody-drug conjugates.

Erdafitinib (JNJ-42756493) is a quinoxaline derivative compound, acts on FGFR1/2/3/4.

AZD4547, a new-type specific FGFR inhibitor, targets for FGFR1/2/3 (IC50: 0.2/2.5/1.8 nM in cell-free assays).

Futibatinib (FGFR-IN-1) is a novel, potent and highly selective FGFR inhibitor, used for antitumor treatment.

Derazantinib (ARQ-087) (ARQ-087) is an ATP competitive tyrosine kinase inhibitor. It exhibits potent activity against FGFR1/FGFR2/FGFR3 chondrocytes (IC50s: 4.5 nM/1.8 nM/4.5 nM).

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.

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.

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

FIIN-1 (FGFR irreversible inhibitor-1) is an irreversible and selective FGFR inhibitor with Kd of 2.8, 6.9, 5.4, 120, 32 and 120 nM for FGFR1, FGFR2, FGFR3, FGFR4, Flt1, Flt14, respectively.FIIN-1 inhibited FGFR1, FGFR2, FGFR3, FGFR4, with IC50 of 9.2, 6.2, 11.9 and 189 nM. FIIN-1 inhibited FGFR1, FGFR2, FGFR3 and FGFR4, with IC50s of 9.2, 6.2, 11.9 and 189 nM, respectively.

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).

TG 100801 is a dual inhibitor of VEGFr2 and Src family (Src and YES) kinases and is a candidate compound for the treatment of age-related macular degeneration (AMD).

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.

Picrasidine Q has the capacity of anti-cell transformation and anti-cancer, it might be a chemopreventive and chemotherapeutic agent by direct targeting FGFR2 and inhibiting cell proliferation of ESCC cells.

TG 100572 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).

FGFR-IN-8 is a potent, orally active FGFR inhibitor that inhibits both wild-type and mutant FGFR. FGFR-IN-8 acts on FGFR1 (IC50<0.5 nM), V564F-FGFR2 (IC5016: 189.1 nM), N549H-FGFR2 (IC50<0.5 nM), V555M-FGFR3 (IC50: 22.6 nM), FGFR3 (IC50<0.5 nM) and FGFR 4 (IC50: 7.30 nM), V555M-FGFR3 (IC50: 22.6 nM), FGFR3 (IC50<0.5 nM) and FGFR 4 (IC50: 7.30 nM). FGFR-IN-8 induces apoptosis and exhibits anti-cancer effects.

Ki23057 is a a FGFR2 inhibitor, which enhances the chemosensitivity of drug-resistant gastric cancer cell lines when used in combination with chemotherapeutic drugs. Ki23057 might be therapeutically promising for treating drug-resistant gastric cancer cells, especially when used in combination with SN38, PTX, or VP16. The apoptosis process might be the main mechanism underlying the synergistic effect of these combinations. The ERCC1 and p53 genes may play an integral role in the synergism between Ki23057 and chemotherapeutic agents in drug-resistant cell lines. (source: Cancer Lett. 2011 Aug 1;307(1):47-52).

LY2874455 has been used in trials studying the treatment of Advanced Cancer.

S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3, blocking cellular phosphorylation of MET, AXL, and FGFRs.

Infigratinib phosphate (BGJ-398 phosphate) is an effective inhibitor of the FGFR family (IC50: 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively).

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

ODM-203, a Selective Inhibitor of FGFR and VEGFR, Shows Strong Antitumor Activity, and Induces Antitumor Immunity

FIIN-3 is an irreversible inhibitor of FGFR.

E-7090 is a fibroblast growth factor receptor inhibitor. E-7090 is a selective inhibitor of the tyrosine kinase activities of FGFR1, -2, and -3.

CPL304110 is an orally active, selective and potent inhibitor of the fibroblast growth factor receptor FGFR (1-3), acting on FGFR1 (IC50: 0.75 nM), FGFR2 (IC50: 0.5 nM), FGFR3 (IC50: 3.05 nM).

HDAC-IN-50, a potent, orally active inhibitor targeting both FGFR (Fibroblast Growth Factor Receptor) and HDAC (Histone Deacetylase), exhibits IC50 values of 0.18, 1.2, 0.46, 1.4, 1.3, 1.6, 2.6, 13 nM for FGFR1, FGFR2, FGFR3, FGFR4, HDAC1, HDAC2, HDAC6, HDAC8, respectively. This dual inhibitor induces apoptosis and cell cycle arrest at the G0/G1 phase while decreasing the expression of phosphorylated FGFR1 (pFGFR1), phosphorylated ERK (pERK), and phosphorylated STAT3 (pSTAT3), thus demonstrating anti-tumor activity.

FGFR-IN-9 is a potent, reversible, and orally active inhibitor of the fibroblast growth factor receptor (FGFR) family, demonstrating IC50 values of 17.1 nM for FGFR4 WT, 29.6 nM for FGFR3, 30.7 nM for FGFR4 V550L, 46.7 nM for FGFR2, and 64.3 nM for FGFR1, respectively.

3-Methylthienyl-carbonyl-JNJ-7706621 is a highly potent and selective inhibitor of cyclin-dependent kinase (CDK). It exhibits impressive IC50 values of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. Additionally, 3-Methylthienyl-carbonyl-JNJ-7706621 demonstrates potent inhibition against GSK-3 (IC50 = 0.041 μM) and moderate potency towards CDK4, VEGF-R2, and FGF-R2 (IC50 = 0.11 μM, 0.13 μM, and 0.22 μM, respectively). Its applications in cancer research are noteworthy.

S49076 HCl (S-49076 Hydrochloride) is an effective inhibitor of MET, AXL/MER, and FGFR1/2/3. S49076 HCl potently blocked cellular phosphorylation of MET, AXL, and FGFRs and inhibited downstream signaling in vitro and in vivo. In cell models, S49076 HCl inhibited the proliferation of MET- and FGFR2-dependent gastric cancer cells blocked MET-driven migration of lung carcinoma cells, and inhibited colony formation of hepatocarcinoma cells expressing FGFR1/2 and AXL. In tumor xenograft models, a good pharmacokinetic/pharmacodynamic relationship for MET and FGFR2 inhibition following oral administration of S49076 HCl was established and correlated well with impact on tumor growth.

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.

Zoligratinib (CH5183284) is a selective and orally available FGFR inhibitor, which is for FGFR1(IC50=9.3 nM), FGFR2(IC50=7.6 nM), FGFR3(IC50=290), and FGFR4(IC50=22 nM), respectively.

ASP5878 potently inhibited the tyrosine kinase activities of recombinant FGFR1, 2, 3, and 4 with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L.

PRN1371 is a specific and potent FGFR1-4 and CSF1R inhibitor (IC50s: 0.6/1.3/4.1/19.3/8.1 nM for FGFR1/2/3/4 and CSF1R).

Nintedanib-13C-d3 is the 13C and deuterated compound of Nintedanib. Nintedanib has a CAS number of 656247-17-5. Nintedanib is an inhibitor of the receptor tyrosine kinases VEGFR/FGFR/PDGFR (IC50s: 13-34/37-610/59/65 nM for VEGFR1-3, FGFR1-4, and PDGFRα/β, respectively).

PHM16 is an ATP competitive FAK and FGFR2 inhibitor.

FGFR4-IN-10 (compound 5a) is a selective and potent inhibitor of FGFR4 (IC50: 70.7 nM).FGFR4-IN-10 does not inhibit other FGFR family members (i.e., FGFR1, FGFR2, and FGFR3).

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.

FGFR-IN-2 (compound 1) is a potent inhibitor of FGFR, acting on FGFR1 (IC50: 7.3 nM), FGFR2 (IC50: 4.3 nM), FGFR3 (IC50: 7.6 nM) and FGFR4 (IC50: 11 nM).

ARQ 069 (3.8-60 μM; for 2 hours) reduces the degree of phosphorylation of FGFR (predominantly FGFR2) in a concentration-dependent manner, without decreasing β-actin. ARQ 069 shows an affinity for FGFR2 of 5.2 μM. ARQ 069 inhibits FGFR phosphorylation in K

FGFR-IN-1 is a highly effective inhibitor targeting the Fibroblast Growth Factor Receptor (FGFR) group, comprising FGFR1, FGFR2, and FGFR3, with an impressive inhibitory concentration (IC 50) of less than 100 nM (US20130338134A1, example 219).

Deruxtecan Analog 2 (example 9 P3), a Deruxtecan derivative, serves as an agent-linker conjugate integrating Camptothecin (CPT), a Topo I inhibitor active against colorectal, breast, lung, and ovarian cancers, with a distinct linker. This analog is employed in synthesizing anti-FGFR2 ADC [1].

AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor ( IC 50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation.

LY2784544(Gandotinib (LY2784544)) is a potent JAK2 inhibitor (IC50: 3 nM), effective in JAK2V617F(Ki: 0.245 nM). The selectivity is higher 8- and 20-fold than JAK1 and JAK3.

Surfen dihydrochloride (Aminoquinuride dihydrochloride) is a potent small molecule antagonist of heparin sulfate with antibacterial and antiviral activity, and inhibits anthrax lethal factor, coagulation factor X, and lethal factor.Surfen inhibits the anticoagulant activity of both normal and low-molecular-weight heparin and inhibits heparin sulfation and heparin cleavage enzyme degradation.Surfen inhibits the blockade of FGF2 binding and signaling mediated by heparin acetylsulfate. Surfen inhibits the blockade of acetylheparin sulfate-mediated FGF2 binding and signaling.Surfen inhibits SEVI and semen-mediated enhancement of HIV type 1 infection.

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

Nintedanib-d8 is a deuterated compound of Nintedanib. Nintedanib has a CAS number of 656247-17-5. Nintedanib is an inhibitor of the receptor tyrosine kinases VEGFR/FGFR/PDGFR (IC50s: 13-34/37-610/59/65 nM for VEGFR1-3, FGFR1-4, and PDGFRα/β, respectively).

FGFR-IN-11 (compound I-5) is an orally active, covalent inhibitor of FGFR, exhibiting IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4). This compound demonstrates nanomolar potency in inhibiting proliferation of various cancer cells and significantly hinders tumor growth in xenograft mouse models [1].