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FGFR2 inhibitor

" in MedChemExpress (MCE) Product Catalog:

68

Inhibitors & Agonists

7

Natural
Products

4

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-145231
    FGFR2-IN-2

    		FGFR Cancer
    FGFR2-IN-2 (Compound 38) is a selective FGFR2 inhibitor with IC50s of 389, 29, and 758 nM for FGFR1, FGFR2, and FGFR3, respectively .
    FGFR2-IN-2
  • HY-162865
    FGFR2-IN-3

    		FGFR Cancer
    FGFR2-IN-3 is an inhibitor of fibroblast growth factor receptor 2 (FGFR2). FGFR2-IN-3 has good binding properties, forming key interactions and inducing conformational changes in FGFR2. FGFR2-IN-3 can be used for research on tumors .
    FGFR2-IN-3
  • HY-145230
    FGFR2-IN-1

    		FGFR Others
    FGFR2-IN-1 is a selective FGFR2 inhibitor with an IC50 of 140 nM.
    FGFR2-IN-1
  • HY-149843
    LC-MB12

    		FGFR PROTACs Cancer
    LC-MB12 is an orally active PROTAC compound targets FGFR2 degradation with a DC50 of 11.8 nM. LC-MB12 contains BGJ398 (a FGFR2 inhibitor), PROTAC linker and CRBN.LC-MB12 inhibits FGFR2 signaling in gastric cancer cells and has anti-tumor activity .
    LC-MB12
  • HY-163620
    LHQ490

    		FGFR Apoptosis Cancer
    LHQ490 is a selective FGFR2 inhibitor, with an IC50 of 5.2 nM. LHQ490 efficiently inhibits the proliferation of BaF3-FGFR2 cells with an IC50 value of 1.4 nM. LHQ490 inhibits FGFR2-driven cancer cell proliferation and induces apoptosis of FGFR2-driven cancer cells .
    LHQ490
  • HY-170919
    FGFR2/3-IN-2

    		FGFR Cancer
    FGFR2/3-IN-2 (compound 10) is an orally active FGFR2 and FGFR3 inhibitor. FGFR2/3-IN-2 inhibits FGFR2 and FGFR3 with IC50s of 3.7 nM and 31.2 nM (preincubation time 1 h), respectively. FGFR2/3-IN-2 spares FGFR1/4 and other kinases without causing diarrhea and serum phosphate elevation in vivo. FGFR2/3-IN-2 induces tumor stasis or regression in the SNU-16 gastric cancer model .
    FGFR2/3-IN-2
  • HY-170934
    BW710

    		FGFR Cancer
    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 .
    BW710
  • HY-163985
    PROTAC FGFR2 degrader 1

    		PROTACs FGFR Apoptosis Cancer
    PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2 IC50 is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cell cycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2. PROTAC FGFR2 degrader 1 inhibits gastric cancer cells remained above 50% at a concentration of 0.17 nM. PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model (Structure Note: Pink, FGFR2 activator: HY-18708; Blue, E3 ligase ligand: HY--10984; Black, linker: HY-163989; E3 ligase ligand + linker：HY-163986) .
    PROTAC FGFR2 degrader 1
  • HY-123134
    FIIN-4

    		FGFR Cancer
    FIIN-4 is a first-in-class, orally active and covalent FGFR inhibitor with IC50s of 2.6 nM, 2.6 nM, 5.6 nM, 9.2 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. FIIN-4 can inhibit metastatic tumor growth.
    FIIN-4
  • HY-151903S
    FGFR2/3-IN-1

    		FGFR Cancer
    FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC50s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC50s of 2.7 nM and 6.1 nM, respectively[1].
    FGFR2/3-IN-1
  • HY-147250A
    Lirafugratinib hydrochloride

    RLY-4008 hydrochloride

    		 FGFR Cancer
    Lirafugratinib (RLY-4008) hydrochloride is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC50 of 3 nM. Lirafugratinib hydrochloride covalently binds to Cys491. Lirafugratinib hydrochloride targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .
    Lirafugratinib hydrochloride
  • HY-147250
    Lirafugratinib

    RLY-4008

    		 FGFR Cancer
    Lirafugratinib (RLY-4008) is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC50 of 3 nM. Lirafugratinib covalently binds to Cys491. Lirafugratinib targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .
    Lirafugratinib
  • HY-N0183
    Formononetin
    10+ Cited Publications

    Biochanin B; Flavosil; Formononetol

    		 FGFR Apoptosis Cardiovascular Disease Cancer
    Formononetin is a potent FGFR2 inhibitor with an IC50 of ~4.31 μM. Formononetin potently inhibits angiogenesis and tumor growth .
    Formononetin
  • HY-101544
    ARQ 069

    		FGFR Cancer
    ARQ 069, an analog of ARQ 523, inhibits FGFR in an enantiospecific manner. ARQ 069 targets the unphosphorylated, inactive forms of FGFR1/FGFR2 kinases (IC50s of 0.84 μM and 1.23 μM, respectively). ARQ 069 inhibits FGFR1/FGFR2 autophosphorylation (IC50s of 2.8 and 1.9 μM, respectively) through a mechanism in a non-ATP competitive dependent manner .
    ARQ 069
  • HY-17601
    Alofanib
    4 Publications Verification

    RPT835

    		 FGFR Apoptosis Cardiovascular Disease Cancer
    Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer and antiangiogenic activity .
    Alofanib
  • HY-117595
    PHM16

    		FAK FGFR Apoptosis Cancer
    PHM16 is an ATP competitive inhibitor of FAK and FGFR2 (IC50: 0.4 μM and 0.37 μM, respectively), with direct potent anti-angiogenic activity .
    PHM16
  • HY-18602
    FIIN-2

    		FGFR Cancer
    FIIN-2 is an irreversible inhibitor of FGFR with an IC50 of 3.1, 4.3, 27, and 45 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
    FIIN-2
  • HY-145043
    FGFR-IN-1

    		FGFR Cancer
    FGFR-IN-1 is a potent FGFR inhibitor with an IC50 of <100 nM for FGFR1, FGFR2, and FGFR3, respectively (patent US20130338134A1, example 219) .
    FGFR-IN-1
  • HY-N0060
    Ferulic acid
    5+ Cited Publications

    Coniferic acid

    		 FGFR Endogenous Metabolite Cancer
    Ferulic acid is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC50s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively.
    Ferulic acid
  • HY-N0060A
    Ferulic acid sodium
    5+ Cited Publications

    Coniferic acid sodium

    		 FGFR Endogenous Metabolite Reactive Oxygen Species Cardiovascular Disease Cancer
    Ferulic acid sodium is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC50s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively.
    Ferulic acid sodium
  • HY-18603
    FIIN-3

    		EGFR FGFR Cancer
    FIIN-3 is an irreversible inhibitor of FGFR with an IC50 of 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
    FIIN-3
  • HY-162577
    FGFR-IN-14

    		FGFR Cancer
    FGFR-IN-14 (compound 10h) is a pan-FGFR inhibitor. FGFR-IN-14 inhibits FGFR1, FGFR2, FGFR3 and FGFR2 V564F gatekeeper mutant with IC50s of 46, 41, 99, and 62 nM, respectively. FGFR-IN-14 strongly suppresses NCI-H520 lung cancer cells, SNU-16 and KATO III gastric cancer cells proliferation with IC50s of 19, 59, and 73 nM, respectively .
    FGFR-IN-14
  • HY-13304
    LY2874455
    3 Publications Verification

    		 FGFR Cancer
    LY2874455 is a pan-FGFR inhibitor with IC50s of 2.8, 2.6, 6.4, 6 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively.
    LY2874455
  • HY-156632
    Resigratinib

    KIN-3248

    		 FGFR Cancer
    Resigratinib (KIN-3248) is an irreversible and orally active covalent inhibitor of FGFR1-4 that effectively inhibits wild-type and drug-resistant mutations (such as FGFR2 V565F, FGFR3 V555M). Resigratinib covalently binds to the Cys492 site of FGFR, blocks the FGFR signaling pathway, inhibits tumor cell proliferation and induces apoptosis. Resigratinib can be used for the study of FGFR2/3-driven solid tumors (such as cholangiocarcinoma and bladder cancer) .
    Resigratinib
  • HY-N0183R
    Formononetin (Standard)

    		FGFR Apoptosis Cardiovascular Disease Cancer
    Formononetin (Standard) is the analytical standard of Formononetin. This product is intended for research and analytical applications. Formononetin is a potent FGFR2 inhibitor with an IC50 of ~4.31 μM. Formononetin potently inhibits angiogenesis and tumor growth .
    Formononetin (Standard)
  • HY-19957
    Zoligratinib
    3 Publications Verification

    Debio 1347; CH5183284

    		 FGFR Cancer
    Zoligratinib (Debio 1347) is an orally available and selective FGFR inhibitor with IC50s of 9.3, 7.6, and 22 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
    Zoligratinib
  • HY-101466
    E7090

    		FGFR Cancer
    E7090 is an orally available, potent, and selective FGFR inhibitor with IC50s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/FGFR2/FGFR3/FGFR4, respectively .
    E7090
  • HY-100818
    Futibatinib
    3 Publications Verification

    TAS-120

    		 FGFR Cancer
    Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM) .
    Futibatinib
  • HY-13034
    Gandotinib
    3 Publications Verification

    LY2784544

    		 JAK FLT3 FGFR VEGFR Cancer
    Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM. Gandotinib (LY2784544) also inhibits FLT3, FLT4, FGFR2, TYK2, and TRKB with IC50 of 4, 25, 32, 44, and 95 nM.
    Gandotinib
  • HY-13330
    Fexagratinib
    25+ Cited Publications

    AZD4547; ADSK091

    		 FGFR Cancer
    Fexagratinib (AZD4547; ADSK091) is a potent inhibitor of the FGFR family with IC50s of 0.2 nM, 2.5 nM, 1.8 nM, and 165 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
    Fexagratinib
  • HY-13311A
    Infigratinib phosphate
    Maximum Cited Publications
    33 Publications Verification

    BGJ-398 phosphate; NVP-BGJ398 phosphate

    		 FGFR Cancer
    Infigratinib phosphate (BGJ-398 phosphate; NVP-BGJ398 phosphate) is a potent inhibitor of the FGFR family with IC50 of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
    Infigratinib phosphate
  • HY-13311S
    Infigratinib-d3

    BGJ-398-d3; NVP-BGJ398-d3

    		 FGFR Cancer
    Infigratinib-d3 is a deuterated analog of infigratinib. Infigratinib is an effective inhibitor of the FGFR family, with IC50 values of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively .
    Infigratinib-d3
  • HY-13311
    Infigratinib
    Maximum Cited Publications
    33 Publications Verification

    BGJ-398; NVP-BGJ398

    		 FGFR Apoptosis Cancer
    Infigratinib (BGJ-398; NVP-BGJ398) is a potent inhibitor of the FGFR family with IC50s of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
    Infigratinib
  • HY-168286
    FGFR-IN-16

    		FGFR Cancer
    FGFR-IN-16 (compound 7N) is a potent inhibitor of FGFR1, FGFR2, and FGFR4, with the IC50s of 8 nM, 4 nM and 3.8 nM, respectively. FGFR-IN-16 plays an important role in cancer research 1].
    FGFR-IN-16
  • HY-100818R
    Futibatinib (Standard)

    		FGFR Cancer
    Futibatinib (Standard) is the analytical standard of Futibatinib. This product is intended for research and analytical applications. Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM) .
    Futibatinib (Standard)
  • HY-19981B
    Derazantinib dihydrochloride

    ARQ-087 dihydrochloride

    		 EGFR Cancer
    Derazantinib (ARQ-087) dihydrochloride is an ATP competitive and orally activeFGFR inhibitor (IC50s: 1.8 nM for FGFR2, 4.5 nM for FGFR1 and 3). Derazantinib dihydrochloride inhibits FGFR phosphorylation. Derazantinib dihydrochloride inhibits tumor growth in multiple xenograft models .
    Derazantinib dihydrochloride
  • HY-19981
    Derazantinib
    1 Publications Verification

    ARQ-087

    		 FGFR Cancer
    Derazantinib (ARQ-087) is an ATP competitive and orally activeFGFR inhibitor (IC50s: 1.8 nM for FGFR2, 4.5 nM for FGFR1 and 3 nM). Derazantinib inhibits FGFR phosphorylation. Derazantinib inhibits tumor growth in multiple xenograft models .
    Derazantinib
  • HY-148779
    FGFR3-IN-5

    		FGFR Cancer
    FGFR3-IN-5 is a potent and selective FGFR3 inhibitor with IC50 values of 3, 44, and 289 nM for FGFR3, FGFR2, and FGFR1, respectively. FGFR3-IN-5 can be used in research of cancer .
    FGFR3-IN-5
  • HY-N0060S1
    Ferulic acid-13C3

    		Isotope-Labeled Compounds FGFR Endogenous Metabolite Cancer
    Ferulic acid- 13C3 is the 13C-labeled Ferulic acid. Ferulic acid is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC50s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively.
    Ferulic acid-13C3
  • HY-150652
    FGFR-IN-8

    		FGFR Apoptosis Cancer
    FGFR-IN-8 (Compound 17a) is a highly potent and orally active panFGFR inhibitor against wild-type and mutant FGFRs. FGFR-IN-8 shows inhibition with IC50 values of <0.5, 189.1, <0.5, 22.6, <0.5 and 7.30 nM against FGFR1, V564F-FGFR2, N549H-FGFR2, V555M-FGFR3, FGFR3 and FGFR4, respectively. GFR-IN-8 induces cancer cell apoptosis and shows anticancer activities .
    FGFR-IN-8
  • HY-109099
    Pemigatinib
    10+ Cited Publications

    INCB054828

    		 FGFR Cancer
    Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma .
    Pemigatinib
  • HY-N0060R
    Ferulic acid (Standard)

    		FGFR Endogenous Metabolite Cancer
    Ferulic acid (Standard) is the analytical standard of Ferulic acid. This product is intended for research and analytical applications. Ferulic acid is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC50s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively.
    Ferulic acid (Standard)
  • HY-101466A
    E7090 succinate

    		FGFR Cancer
    E7090 succinate is an orally available, selective and potent inhibitor of FGFR1, FGFR2 and FGFR3 tyrosine kinase activities, with IC50 values of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/2/3/4, respectively .
    E7090 succinate
  • HY-15391
    Lucitanib
    5+ Cited Publications

    E-3810

    		 VEGFR FGFR Cancer
    Lucitanib (E-3810) is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively .
    Lucitanib
  • HY-15391A
    Lucitanib dihydrochloride

    		VEGFR FGFR Cancer
    Lucitanib (E-3810) dihydrochloride is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively .
    Lucitanib dihydrochloride
  • HY-142921
    FGFR-IN-2

    		FGFR Cancer
    FGFR-IN-2 (compound 1) is a potent FGFR inhibitor with IC50s of 7.3 nM, 4.3 nM, 7.6 nM, 11 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. FGFR-IN-2 has the potential for cancer research .
    FGFR-IN-2
  • HY-N7715
    Ferulic acid acyl-β-D-glucoside

    Ferulic acid glucoside

    		 Drug Metabolite Others
    Ferulic acid acyl-β-D-glucoside is a metabolite of Ferulic Acid (HY-N0060) . Ferulic acid is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC50s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively .
    Ferulic acid acyl-β-D-glucoside
  • HY-146541
    FGFR4-IN-10

    		FGFR Cancer
    FGFR4-IN-10 (compound 5a) is a potent and selective FGFR4 inhibitor with an IC50 value of 70.7 nM. FGFR4-IN-10 shows no inhibition against other FGFR family members, i.e. FGFR1, FGFR2 and FGFR3 .
    FGFR4-IN-10
  • HY-N9507
    Picrasidine Q

    		Apoptosis FGFR Cancer
    Picrasidine Q, an alkaloid component extracted from Angelica keiskei species, has the capacity of anti-cell transformation and anti-cancer. Picrasidine Q induces cell apoptosis and G1 phase arrest in human esophageal cancer cell lines, and directly inhibits FGFR2 kinase activity .
    Picrasidine Q
  • HY-152104
    FGFR-IN-9

    		FGFR Cancer
    FGFR-IN-9 (Compound 19) is a potent, reversible and orally active FGFR inhibitor with an IC50 of 17.1, 29.6, 30.7, 46.7 and 64.3 nM against FGFR4 WT, FGFR3, FGFR4 V550L, FGFR2 and FGFR1, respectively .
    FGFR-IN-9

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