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FGFR

The fibroblast growth factor receptors (FGFR) are, as their name implies, receptors that bind to members of the fibroblast growth factor (FGF) family of proteins. Some of these receptors are involved in pathological conditions. For example, a point mutation in FGFR3 can lead to achondroplasia.

  • AZD4547
    T19481035270-39-3
    AZD4547, a new-type specific FGFR inhibitor, targets for FGFR1/2/3 (IC50: 0.2/2.5/1.8 nM in cell-free assays).
    • $33
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  • Erdafitinib
    T37261346242-81-6
    Erdafitinib (JNJ-42756493) is a quinoxaline derivative compound, acts on FGFR1/2/3/4.
    • $39
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  • Futibatinib
    T50441448169-71-8
    Futibatinib (FGFR-IN-1) is a novel, potent and highly selective FGFR inhibitor, used for antitumor treatment.
    • $53
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  • Derazantinib
    TQ02281234356-69-4
    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).
    • $52
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  • Lenvatinib
    T0520417716-92-8
    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.
    • $40
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  • Fisogatinib
    T34561707289-21-1
    Fisogatinib (BLU-554) is a potent inhibitor of fibroblast growth factor receptor 4 (FGFR4).
    • $51
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  • Ferulic Acid
    T22151135-24-6
    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.
    • $30
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  • Nintedanib
    T1777656247-17-5
    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.
    • $38
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  • Pazopanib
    T0097L444731-52-6
    Pazopanib (GW786034), a small molecule inhibitor, inhibits multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits VEGFR-1, -2 and -3, c-kit and PDGF-R, which may result in inhibition of angiogenesis in tumors in which these receptors are upregulated.
    • $42
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  • Formononetin
    T0724485-72-3
    Formononetin (Flavosil) is an O-methylated isoflavone and a phytoestrogen from the root of Astragalus membranaceus.
    • $45
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  • Amlexanox
    T163968302-57-8
    Amlexanox (AA673) is an anti-aphthous ulcer drug. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mast cells, neutrophils, and mononuclear cells. Amlexanox also acts as a leukotriene D4 antagonist and a phosphodiesterase inhibitor. Amlexanox decreases the time ulcers take to heal as well as the pain associated with the ulcers.
    • $32
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  • CP-547632
    T10870L252003-65-9In house
    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.
    • $30
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  • FGFR2-IN-1
    T613042677709-76-9
    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
    • $56
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  • SM27
    T248046266-54-2In house
    SM27 is a fibroblast growth factor 2 (FGF2) inhibitor with anti-angiogenic activity and can be used to study tumours.
    • $195
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  • FIIN-4
    T273192093088-81-2In house
    FIIN-4 is a covalent inhibitor of FGFR and can be used in studies about metastatic breast cancer.
    • $329
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  • FIIN-1
    T374261256152-35-8In house
    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.
    • $72
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  • CP-547632 hydrochloride
    T10870252003-71-7In house
    CP-547632 hydrochloride is a well-tolerated and orally-bioavailable inhibitor of the VEGFR-2 and basic FGF kinases (IC50s: 11 nM and 9 nM) with antitumor efficacy.
    • $44
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  • ZM323881 hydrochloride
    T1991193000-39-4In house
    ZM323881 hydrochloride (ZM 323881 HCl) is a potent and selective VEGFR2 inhibitor.
    • $66
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  • TG 100572 Hydrochloride
    T13156L867331-64-4In house
    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).
    • $399
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  • Danusertib
    T2094827318-97-8
    Danusertib (PHA-739358) is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in tumor cells in which Aurora kinases are overexpressed.
    • $54
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  • Mubritinib
    T6124366017-09-6
    Mubritinib (TAK-165) (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM.
    • $32
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  • PHA-665752
    T6128477575-56-7
    PHA-665752 is an effective, specific and ATP-competitive c-Met inhibitor (IC50: 9 nM), >50-fold selectivity for c-Met than STKs or RTKs.
    • $59
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  • Alofanib
    T51221612888-66-0
    Alofanib (RPT835) is a selective allosteric inhibitor of FGFR2 and has a dramatic inhibitory effect on FGF2-induced phosphorylation of FRS2a in KATO III cells (IC50 <10 nM). It has no direct effect on FGF2-dependent FGFR1 and FGFR3 phosphorylation levels in either cell lines and no effects on FGF2-FGFR2 binding.
    • $31
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  • Pemigatinib
    T124011513857-77-6
    Pemigatinib (INCB054828) is an orally active, selective inhibitor of FGFR(IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively).
    • $41
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  • FIIN-2
    T68361633044-56-0
    FIIN-2, an irreversible, pan-FGFR inhibitor, inhibits FGFR1/2/3/4 with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM, respectively.
    • $35
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  • Orantinib
    T6184252916-29-3
    Orantinib (NSC 702827) , a excellent effective against PDGFR autophosphorylation with Ki of 8 nM, also highly inhibits Flk-1 and FGFR1 trans-phosphorylation. It shows little effect against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2 and does not suppresses EGFR.
    • $47
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  • Ferulic acid sodium
    T2S000724276-84-4
    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.
    • $45
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  • Lenvatinib mesylate
    T8541857890-39-2
    Lenvatinib mesylate (E7080 (mesylate)) is an oral and multi-targeted inhibitor of VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, with potent antitumor activities.
    • $34
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  • Roblitinib
    T42351708971-55-4
    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 the activity of FGFR4, which leads to an inhibition of tumor cell proliferation in FGFR4-overexpressing cells. Roblitinib is a receptor tyrosine kinase upregulated in certain tumor cells and involved in tumor cell proliferation, differentiation, angiogenesis, and survival.
    • $53
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  • TAK-632
    T18861228591-30-7
    TAK-632 is a potent pan-Raf inhibitor.
    • $35
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  • Infigratinib
    T1975872511-34-7
    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.
    • $39
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  • Ponatinib
    T2372943319-70-8
    Ponatinib (AP24534) is an orally available, multitargeted kinase inhibitor (IC50s: 0.37/1.1/1.5/2.2/5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively).
    • $50
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  • PD173074
    T2642219580-11-7
    PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold for FGFR1 than PDGFR and c-Src.
    • $36
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  • Resigratinib
    T798562750709-91-0
    Resigratinib (KIN-3248) is a FGFR tyrosine kinase inhibitor exhibiting antineoplastic activity [1].
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  • FGFR3-IN-7
    T824042833703-79-8
    FGFR3-IN-7 is a potent, selective inhibitor of FGFR 3, demonstrating an IC50 value of less than 350 nM , and is utilized in cancer research [1].
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  • FGFR3-IN-6
    T824052833703-72-1
    FGFR3-IN-6 is a potent, selective inhibitor of FGFR 3, exhibiting an IC50 value of less than 350 nM , and is utilized in cancer research [1].
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  • Fazpilodemab
    T783132517935-02-1
    Fazpilodemab (BFKB8488A) is a humanized agonistic bispecific antibody that targets fibroblast growth factor receptor 1c (FGFR1c) and Klothoβ. It is utilized in research pertaining to Type 2 diabetes mellitus (T2DM) and nonalcoholic fatty liver disease (NAFLD) [1].
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  • Bemarituzumab
    T766731952272-74-0
    Bemarituzumab is a novel humanized IgG1 monoclonal antibody targeting FGFR2b. Bemarituzumab prevents FGFR2b from binding to FGF and activation. Potential applications of Bemarituzumab in cancer research.
    • $198
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  • Vofatamab
    T768771312305-12-6
    Vofatamab (B-701) is a fully human monoclonal antibody targeting FGFR3. Vofatamab has potential anticancer and antitumor activity and is often used in combination with other compounds to treat cancer.
    • $339
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  • Irpagratinib
    T798502230974-62-4
    Irpagratinib (ABSK011) is an orally active fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor with specificity for FGFR4, exhibiting an IC50 of less than 10 nM. It effectively inhibits FGFR4 auto-phosphorylation and disrupts subsequent signal transduction to downstream pathways. Demonstrating high exposure in pharmacokinetic studies in mice, rats, and dogs, Irpagratinib also displays antineoplastic activity in subcutaneous xenograft tumor models [1].
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  • S6K2-IN-1
    T79871
    S6K2-IN-1 (Compound 2) is an inhibitor of S6K2 with an IC50 of 22 nM and also exhibits inhibitory activity against FGFR4 with an IC50 of 216 nM. This compound demonstrates acceptable stability in mouse liver microsomes [1].
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  • Masitinib mesylate
    T85441048007-93-7
    Masitinib mesylate (AB-1010 mesylate) is a selective and orally bioavailable c-Kit inhibitor (IC50 of 200 nM,540/800 nM,510 nM for human recombinant c-Kit;PDGFRα/β;LynB,respectively).
    • $30
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  • H3B-6527
    T77381702259-66-2
    H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma, with antineoplastic activity.
    • $64
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  • KHS101 hydrochloride
    T51701784282-12-7
    KHS101 is a TACC3 inhibitor and can selectively induce a neuronal differentiation phenotype.
    • $36
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  • FGFR2-IN-2
    T614732677709-81-6
    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.
    • $78
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  • Mal-amido-PEG2-C2-amido-Ph-C2-CO-AZD
    T164861037589-69-7
    Mal-amido-PEG2-C2-amido-Ph-C2-CO-AZD (PF-05231023) is a long-acting fibroblast growth factor 21 (FGF21) analog and is an FGF21-receptor agonist. It is also suitable for development as a potential treatment for T2DM.
    • $30
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  • EOC317
    T4318939805-30-8
    EOC317 (ACTB-1003) is an oral kinase inhibitor (IC50: 6/2/4 nM, for FGFR1/VEGFR2/Tie-2).
    • $93
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  • PP58
    T13824212391-58-7
    PP58 is an inhibitor of PDGFR, FGFR and Src family.
    • $39
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  • ODM-203
    T76111430723-35-5
    ODM-203, a Selective Inhibitor of FGFR and VEGFR, Shows Strong Antitumor Activity, and Induces Antitumor Immunity
    • $36
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  • PHA-680632
    T6338398493-79-3
    PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2/3.
    • $39
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