2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. FGFR
  5. FGFR1 Isoform
  6. FGFR1 Inhibitor

FGFR1 Inhibitor

FGFR1 Inhibitors (91):

Cat. No. Product Name Effect Purity
  • HY-100315
    XL 999
    		Inhibitor 99.01%
    XL999 is a multi-target tyrosine kinase inhibitor. XL999 has IC50 values for VEGFR2/KDR/Flk-1, Flt-1, FGFR1 and PDGFRα of 4 nM, 20 nM, 4 nM and 2 nM, respectively. XL999 can be used in the research of cancer.
  • HY-12047S
    Ponatinib-d8
    		Inhibitor 99.91%
    Ponatinib-d8 is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2/KDR/Flk-1, FGFR1, and Src, respectively.
  • HY-10184
    TG 100572
    		Inhibitor
    TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1/Flt-1, VEGFR2/KDR/Flk-1, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-B0062
    Dovitinib lactate hydrate
    		Inhibitor
    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/Flt-1/2/3 and PDGFRα/β, respectively.
  • HY-101466A
    E7090 succinate
    		Inhibitor 99.17%
    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.
  • HY-139376
    FGFR1 inhibitor-2
    		Inhibitor
    FGFR1 inhibitor-2 is a FGFR1 inhibitor (IC50 is 4.55 μM in MDA-MB-231 cells). FGFR1 inhibitor-2 can be used for the research of metastatic triple-negative breast cancer.
  • HY-101544
    ARQ 069
    		Inhibitor
    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.
  • HY-142921
    FGFR-IN-2
    		Inhibitor
    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.
  • HY-152104
    FGFR-IN-9
    		Inhibitor
    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 FGFR4WT, FGFR3, FGFR4V550L, FGFR2 and FGFR1, respectively.
  • HY-150652
    FGFR-IN-8
    		Inhibitor
    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.
  • HY-151903S
    FGFR2/3-IN-1
    		Inhibitor
    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].
  • HY-155028
    FGFR-IN-11
    		Inhibitor
    FGFR-IN-11 (compound I-5) is an orally active and covalent FGFR inhibitor with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4), respectively. FGFR-IN-11 inhibits multiple cancer cell proliferation with nanomolar activity. FGFR-IN-11 inhibits tumor growth significantly in xenograft mice models.
  • HY-158248
    FGFR4-IN-19
    		Inhibitor
    FGFR4-IN-19 (compound 8B) is a potent covalent fibroblast growth factor receptor 4 (FGFR4) inhibitor (IC50=1.2 nM). FGFR4-IN-19 achieves high efficiency and isotype selectivity by covalently targeting a rare cysteine (C552) in the FGFR4 kinase domain. FGFR4-IN-19 can be used for hepatocellular carcinoma (HCC) research.
  • HY-150026
    Multi-kinase-IN-2
    		Inhibitor
    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.
  • HY-161995
    FGFR1/VEGFR2-IN-2
    		Inhibitor
    FGFR1/VEGFR2-IN-2 (compound 6l) is a VEGFR2/KDR/Flk-1/FGFR1 dual inhibitor. The IC50 values for VEGFR2/KDR/Flk-1 and FGFR1 are 0.025 µM and 0.026 µM respectively, and for EGFR and PDGFR-β, the IC50 values are 0.106 µM and 0.077 µM. FGFR1/VEGFR2-IN-2 showes significant anti-cancer activity (GI=60.38%) on NCI-60 cell line, with an IC50 of 8.51 µM in T-47D cell line and anti-migration. FGFR1/VEGFR2-IN-2 acts to arrest cells in the G1 phase and promote apoptosis and necrosis; the IC50 for MCF-7 cell line exceeds 100 µM, and the IC50 for MDA-MB-231 is 69.17 µM, non-toxic to normal cells.
  • HY-149415
    Multi-kinase-IN-5
    		Inhibitor
    Multi-kinase-IN-5 (compound 15c) is a promising multi-kinase inhibitory agent. Multi-kinase-IN-5 inhibits a panel of protein kinases (RET, KIT, cMet, VEGFR1/Flt-1,2, FGFR1, PDGFR and BRAF), showing % inhibition of 74%, 31%, 62%, 40%, 73%, 74%, 59%, and 69%, respectively, and IC50 of 1.287, 0.117 and 1.185 μM against FGFR1, VEGFR, and RET kinases, respectively.
  • HY-152146
    HDAC-IN-50
    		Inhibitor
    HDAC-IN-50 is a potent and orally active FGFR and HDAC dual inhibitor with 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. HDAC-IN-50 induces Apoptosis and cell cycle arrest at G0/G1 phase. HDAC-IN-50 decreases the expression of pFGFR1, pERK, pSTAT3. HDAC-IN-50 shows anti-tumor activity.
  • HY-143272
    FGFR1 inhibitor-6
    		Inhibitor
    FGFR1 inhibitor-6 is a potent FGFR1 inhibitor with an IC50 value of 16.31 nM. FGFR1 inhibitor-6 shows cytotoxic activities. FGFR1 inhibitor-6 induces apoptosis and cell cycle arrest at pre-G1 and G2/M phase.
  • HY-168286
    FGFR-IN-16
    		Inhibitor
    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 research1].
  • HY-147715
    FGFR3-IN-3
    		Inhibitor
    FGFR3-IN-3 (compound 40a) is a potent and pan-FGFR inhibitor, with IC50s of 2.1 nM, 3.1 nM, 4.3 nM and 74 nM for FGFR1, 2, 3, and 4, respectively. FGFR3-IN-3 can be used for the research of bladder cancer.