2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. FGFR
  5. FGFR2 Isoform
  6. FGFR2 Inhibitor

FGFR2 Inhibitor

FGFR2 Inhibitors (77):

Cat. No. Product Name Effect Purity
  • 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-N9507
    Picrasidine Q
    		Inhibitor
    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.
  • 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-141685
    3-Methylthienyl-carbonyl-JNJ-7706621
    		Inhibitor
    3-Methylthienyl-carbonyl-JNJ-7706621 is a potent and selective inhibitor of cyclin-dependent kinase (CDK), with IC50s of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. 3-Methylthienyl-carbonyl-JNJ-7706621 also shows potent inhibition of GSK-3 (IC50=0.041 μM) and modest potency against CDK4, VEGF-R2, and FGF-R2 (IC50=0.11, 0.13, 0.22 μM, respectively). 3-Methylthienyl-carbonyl-JNJ-7706621 can be used for the research of cancer.
  • 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-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-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.
  • HY-147713
    FGFR3-IN-1
    		Inhibitor
    FGFR3-IN-1 (compound 1) is a fibroblast growth factor receptor (FGFR) inhibitor, with IC50s of 40 nM, 5.1 nM, and 12 nM for FGFR1, 2, and 3, respectively. FGFR3-IN-1 can be used for the research of bladder cancer.
  • HY-170919
    FGFR2/3-IN-2
    		Inhibitor
    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.
  • HY-165603
    Si5-N14
    		Inhibitor
    Si5-N14 is a key component of siloxane-incorporated lipid nanoparticles (SiLNP), possessing pro-vascular repair and anti-tumor activities. In the transgenic GFP mouse model, Si5-N14 can mediate CRISPR-Cas9 editing. In the Lewis lung carcinoma (LLC) tumor-bearing mouse model, Si5-N14 can knock out the expression of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) to exert an anti-tumor effect. In a mouse model of lung injury induced by viral infection, the delivery of Fibroblast Growth Factor-2 (FGF-2) mRNA via Si5-N14 can promote vascular repair, increase blood oxygen levels, and improve lung function. Si5-N14 shows promise for research in the fields of oncology, pneumonia, and cardiovascular diseases.
  • HY-159642G
    TYRA-300 (GMP)
    		Inhibitor
    TYRA-300 GMP is TYRA-300 (HY-159642) produced by using GMP guidelines. TYRA-300 GMP is an orally active, selective inhibitor for FGFR3 with an IC50 of 11 nM. TYRA-300 GMP exhibits antitumor efficacy against urothelial cancers and solid tumors.
  • HY-164459
    AZ8010
    		Inhibitor
    AZ8010 (AZ12908010) is a potent FGFR1-3 inhibitor. AZ8010 has anti-proliferative activity and can be used for the research of cancer.
  • HY-10187
    TG 100801 Hydrochloride
    		Inhibitor
    TG 100801 Hydrochloride is a proagent that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. 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, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-15599A
    SSR128129E free acid
    		Inhibitor
    SSR128129E free acid is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.
  • HY-15391A
    Lucitanib dihydrochloride
    		Inhibitor
    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.
  • HY-159503A
    Segigratinib hydrochloride
    		Inhibitor
    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.