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FGFRs-IN-1

" in MedChemExpress (MCE) Product Catalog:

73

Inhibitors & Agonists

1

Biochemical Assay Reagents

9

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10981
    Lenvatinib
    Maximum Cited Publications
    92 Publications Verification

    E7080

    VEGFR FGFR PDGFR c-Kit RET Cancer
    Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
    Lenvatinib
  • HY-50904
    Nintedanib
    70+ Cited Publications

    BIBF 1120

    PDGFR VEGFR FGFR Cancer
    Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
    Nintedanib
  • HY-18708
    Erdafitinib
    35+ Cited Publications

    JNJ-42756493

    FGFR Apoptosis Cancer
    Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.
    Erdafitinib
  • HY-11106
    Nintedanib esylate
    70+ Cited Publications

    BIBF 1120 esylate

    PDGFR VEGFR FGFR Cancer
    Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
    Nintedanib esylate
  • HY-50905
    Dovitinib
    10+ Cited Publications

    CHIR-258; TKI258

    FLT3 c-Kit FGFR VEGFR PDGFR c-Fms Cancer
    Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity [1] .
    Dovitinib
  • HY-10981A
    Lenvatinib mesylate
    Maximum Cited Publications
    92 Publications Verification

    E7080 mesylate

    VEGFR FGFR PDGFR RET c-Kit Cancer
    Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
    Lenvatinib mesylate
  • HY-100019
    Rogaratinib
    5+ Cited Publications

    BAY1163877

    FGFR Cancer
    Rogaratinib (BAY1163877) is a potent and selective fibroblast growth factor receptor (FGFR) inhibitor. Rogaratinib inhibits FGFRs with IC50s of 11.2 nM (FGFR1), <1 nM (FGFR2), 18.5 nM (FGFR3), 127 nM (VEGFR3/FLT4), 201 nM (FGFR4), respectively [1] .
    Rogaratinib
  • HY-101466

    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 [1].
    E7090
  • HY-119367

    FGFR VEGFR Cancer
    ODM-203 is an orally active and selective FGFR/VEGFR inhibitor with IC50 values of 6, 11, 16, 5, 9, 26 and 35 nM for FGFR3/1/2 and VEGFR3/2/1/4, respectively. ODM-203 has strong anti-tumour activity and activates immune responses in the tumour microenvironment [1].
    ODM-203
  • HY-10207
    Dovitinib lactate
    10+ Cited Publications

    CHIR-258 lactate; TKI-258 lactate

    FLT3 c-Kit FGFR VEGFR PDGFR Cancer
    Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively [1].
    Dovitinib lactate
  • HY-50904S2

    BIBF 1120-d8

    Isotope-Labeled Compounds PDGFR VEGFR FGFR Cancer
    Nintedanib-d8 is deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
    Nintedanib-d8
  • HY-165298

    PROTACs FGFR ERK Cancer
    DGY-09-192 is a PROTAC FGFR1/2 degrader (FGFR1: DC50 = 4.35 nM; FGFR2: DC50 = 70 nM). DGY-09-192 preferentially degrades wild-type FGFR1/2 and multiple FGFR2 fusion proteins (including FGFR2-PHGDH and FGFR2-OPTN). DGY-09-192 suppresses downstream FGFR signaling (reducing phosphorylation of FRS2 Y196 and ERK1/2 T202/Y204) in vitro and vivo. DGY-09-192 can be used for the study of FGFR-driven cancers. (Pink: FGFR1/2 ligand (HY-160013), Blue: VHL Ligand (HY-112078), Black: Linker (HY-W020017)) [1].
    DGY-09-192
  • HY-10337
    Brivanib
    2 Publications Verification

    BMS-540215

    VEGFR Autophagy Cancer
    Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β [1].
    Brivanib
  • HY-101768
    PRN1371
    1 Publications Verification

    FGFR c-Fms Cancer
    PRN1371 is a highly selective and potent FGFR1-4 and CSF1R inhibitor with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R, respectively [1].
    PRN1371
  • HY-100491

    FGFR Cancer
    H3B-6527 is an orally active, highly selective and covalent FGFR4 inhibitor with an IC50 of <1.2 nM. H3B-6527 has at least 250-fold selectivity over FGFR1-3 with IC50s of 320 nM, 1290 nM and 1060 nM respectively. H3B-6527 has potent anti-cancer activity [1].
    H3B-6527
  • HY-145601

    TT 00420

    Aurora Kinase FGFR VEGFR Cancer
    Tinengotinib (TT00420) is an orally active, spectrally selective small molecule kinase inhibitor targeting Aurora A/B (IC50=1.2-3.3 nM), FGFR1/2/3 (IC50=1.5-3.5 nM), VEGFRs, JAK1/2 and CSF1R. Tinengotinib blocks Aurora kinase-mediated cell cycle progression (inducing G2/M arrest), inhibits FGFR/JNK-JUN signaling pathway and activates MEK/ERK-dependent apoptotic pathway. Tinengotinib has the activity of anti-tumor proliferation, inducing apoptosis, inhibiting angiogenesis and regulating tumor microenvironment. Tinengotinib can be used in the study of triple-negative breast cancer (TNBC), gallbladder cancer and tumor immune microenvironment [1] .
    Tinengotinib
  • HY-12965
    S49076
    1 Publications Verification

    FGFR c-Met/HGFR Cancer
    S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nM.
    S49076
  • HY-10336
    Brivanib (alaninate)
    2 Publications Verification

    BMS-582664

    VEGFR Autophagy Cancer
    Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ [1].
    Brivanib (alaninate)
  • HY-10981S

    E7080-d4

    VEGFR FGFR PDGFR c-Kit RET Cancer
    Lenvatinib-d4 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
    Lenvatinib-d4
  • HY-156632

    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) [1] .
    Resigratinib
  • HY-15813

    FGFR irreversible INhibitor-1

    FGFR Cancer
    FIIN-1 is a potent, irreversible, selective FGFR inhibitor. FIIN-1 binds to FGFR1/2/3/4 and Flt1/4 with Kds of 2.8/6.9/5.4/120 nM and 32/120 nM respectively. The biochemical IC50s of FIIN-1 are 9.2, 6.2, 11.9, and 189 nM against FGFR1/2/3/4, respectively [1].
    FIIN-1
  • HY-163705

    PROTACs FGFR Cancer
    BR-cpd7 is a PROTAC degrader for fibroblast growth factor receptor FGFR1/2 with DC50 of 10 nM. BR-cpd7 arrests cell cycle, inhibits proliferations of FGFR1/2 aberrant activated tumor cells. (Pink: ligand for target protein FGFR-IN-12 (HY-160013); Black: linker; Blue: ligand for E3 ligase Thalidomide-NH-CH2-COOH (HY-131717)) [1]
    BR-cpd7
  • HY-10981R

    E7080 (Standard)

    Reference Standards VEGFR FGFR PDGFR c-Kit RET Cancer
    Lenvatinib (Standard) is the analytical standard of Lenvatinib. This product is intended for research and analytical applications. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
    Lenvatinib (Standard)
  • HY-112345

    FGFR PDGFR EGFR Src Cancer
    PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity [1].
    PD-089828
  • HY-170846

    FGFR VEGFR Bcr-Abl FLT3 Cytochrome P450 Inflammation/Immunology
    FGFRs-IN-1 (Compound A16) is the orally active inhibitor for FGFR, that inhibits FGFR1/2/3/4 with IC50s of 2.3, 7, 11, and 163 nM, respectively. FGFRs-IN-1 also inhibits VEGFR1/2/3, Abl, and Flt3 with IC50s of 61, 176, 112, 26, and 353 nM, respectively. FGFRs-IN-1 exhibits weak inhibitory efficacy against CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and inhibits epithelial-mesenchymal transition (EMT) in TGF1 stimulated A549 cell. FGFRs-IN-1 exhibits anti-inflammatory activity in Bleomycin (HY-17565)-induced mouse pulmonary fibrosis model and CCl4 (HY-Y0298)-induced mouse liver fibrosis model [1].
    FGFRs-IN-1
  • HY-133980A

    Drug Metabolite Cancer
    O-Demethyl Lenvatinib hydrochloride is a metabolite of Lenvatinib (HY-10981). Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET. Lenvatinib shows potent antitumor activities [1] .
    O-Demethyl Lenvatinib hydrochloride
  • HY-50904S1

    BIBF 1120-13C,d3

    Isotope-Labeled Compounds PDGFR VEGFR FGFR Cancer
    Nintedanib- 13C,d3 is the 13C- and deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
    Nintedanib-13C,d3
  • HY-W006833

    Drug Derivative PDGFR FGFR Others
    1-Phenylindole (Compound 8) is a 1-Phenylbenzimidazole analogue. 1-Phenylindole shows IC50 values of >50 μM and >50 μM for PDGFR and FGFR, respectively. 1-Phenylbenzimidazole is a selective PDGFR inhibitor [1].
    1-Phenylindole
  • HY-133980

    Drug Metabolite Cancer
    O-Demethyl Lenvatinib is a metabolite of Lenvatinib (HY-10981). Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
    O-Demethyl Lenvatinib
  • HY-18708R

    JNJ-42756493 (Standard)

    Reference Standards FGFR Apoptosis Cancer
    Erdafitinib (Standard) is the analytical standard of Erdafitinib. This product is intended for research and analytical applications. Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.
    Erdafitinib (Standard)
  • HY-B0062

    TKI258 lactate hydrate; CHIR-258 lactate hydrate

    FLT3 c-Kit FGFR VEGFR PDGFR Cancer
    Dovitinib lactate hydrate (TKI258 lactate hydrate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively [1].
    Dovitinib lactate hydrate
  • HY-50904S

    BIBF 1120-d3

    PDGFR VEGFR FGFR Cancer
    Nintedanib-d3 is the deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
    Nintedanib-d3
  • HY-50904R

    BIBF 1120 (Standard)

    Reference Standards PDGFR VEGFR FGFR Cancer
    Nintedanib (Standard) is the analytical standard of Nintedanib. This product is intended for research and analytical applications. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
    Nintedanib (Standard)
  • HY-11106R

    BIBF 1120 esylate (Standard)

    Reference Standards PDGFR VEGFR FGFR Cancer
    Nintedanib esylate (Standard) is the analytical standard of Nintedanib esylate. This product is intended for research and analytical applications. Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
    Nintedanib esylate (Standard)
  • HY-151903S

    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-50905R

    CHIR-258 (Standard); TKI258 (Standard)

    FLT3 c-Kit FGFR VEGFR PDGFR c-Fms Reference Standards Cancer
    Dovitinib (Standard) is the analytical standard of Dovitinib. This product is intended for research and analytical applications. Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity [1] .
    Dovitinib (Standard)
  • HY-145043

    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) [1].
    FGFR-IN-1
  • HY-147621

    FGFR Cancer
    FGFR-IN-6 (Compound 5) is a FGFR inhibitor . FGFR-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    FGFR-IN-6
  • HY-148778

    FGFR Cancer
    FGFR3-IN-4 is a selective FGFR3 inhibitor, with an IC50 value of less than 50 nM. FGFR3-IN-4 is at least 10 fold more selective for FGFR3 than for FGFR1 .
    FGFR3-IN-4
  • HY-101466A

    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 [1].
    E7090 succinate
  • HY-10981S1

    E7080-d5

    VEGFR FGFR PDGFR c-Kit RET Cancer
    Lenvatinib-d5 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
    Lenvatinib-d5
  • HY-10981AR

    E7080 mesylate (Standard)

    Reference Standards VEGFR FGFR PDGFR RET c-Kit Cancer
    Lenvatinib (mesylate) (Standard) is the analytical standard of Lenvatinib (mesylate). This product is intended for research and analytical applications. Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
    Lenvatinib mesylate (Standard)
  • HY-60218

    Biochemical Assay Reagents Drug Intermediate Cancer
    1-Boc-3-(hydroxymethyl)pyrrolidine is an intermediate. 1-Boc-3-(hydroxymethyl)pyrrolidine can be used to synthesize a FGFR1/2/3/4 inhibitor (Compound 2). 1-Boc-3-(hydroxymethyl)pyrrolidine can be used in cancer research [1].
    1-Boc-3-(hydroxymethyl)pyrrolidine
  • HY-10981S2

    E7080-15N,d4

    VEGFR c-Kit FGFR RET PDGFR Isotope-Labeled Compounds Cancer
    Lenvatinib- 15N,d4 is 15N and deuterated labeled Lenvatinib (HY-10981). Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
    Lenvatinib-15N,d4
  • HY-159503A

    3D185; HH185

    FGFR c-Fms Cancer
    Segigratinib hydrochloride (3D185) is a potent inhibitor of FGFR1/2/3 and CSF-1R; The IC50 values for FGFR1, FGFR2, FGFR3 and CSF-1R are 0.5, 1.3, 3.6 and 3.8 nM, respectively. Segigratinib hydrochloride has antitumor activity [1].
    Segigratinib hydrochloride
  • HY-10207R

    CHIR-258 lactate (Standard); TKI-258 lactate (Standard)

    Reference Standards FLT3 c-Kit FGFR VEGFR PDGFR Cancer
    Dovitinib (lactate) (Standard) is the analytical standard of Dovitinib (lactate). This product is intended for research and analytical applications. Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively [1].
    Dovitinib lactate (Standard)
  • HY-50905S

    FLT3 c-Kit FGFR VEGFR PDGFR c-Fms Cancer
    Dovitinib-d8 is the deuterium labeled Dovitinib. Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively [1] .
    Dovitinib-d8
  • HY-174154

    FGFR Cancer
    INCB126503 is an orally activeM, selective FGFR2/3 Inhibitor with IC50 values of 70 nM (FGFR1), 2.1 nM (FGFR2), 1.2 nM (FGFR3), 0.92 nM (FGFR3-V555L), 0.85 nM (FGFR3-V555M) and 64 nM (FGFR4). INCB126503 suppresses FGFR signaling in vivo without causing hyperphosphatemia and shows antitumor efficacy in xenograft models harboring FGFR3 genetic alterations [1].
    INCB126503
  • HY-150026

    VEGFR PDGFR FGFR c-Kit Akt Src Apoptosis Cancer
    Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity [1].
    Multi-kinase-IN-2
  • HY-160013

    FGFR Cancer
    FGFR-IN-12 (example 14), a pyrimidinyl aryl urea derivative, is a potent FGFR inhibitor .
    FGFR-IN-12

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