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Catalog No.
Product Name
Application
Product Information
Citations
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FGFR Inhibitor
FGFR-IN-22 is a potent FGFR inhibitor, demonstrating IC50 values of 0.631 nM for FGFR1, 1.26 nM for FGFR2, 0.851 nM for FGFR3, and 1 nM for FGFR4. This compound effectively inhibits cell proliferation linked to FGFR1 and FGFR3 signaling pathways, making it a valuable tool for research in cancer types such as chronic lymphocytic leukemia (CLL). FGFR-IN-22 is useful for studying the role of FGFRs in tumor biology and therapeutic development. -
FGFR4 Inhibitor
FGFR4-IN-6 is a covalent, reversible inhibitor of Fibroblast Growth Factor Receptor 4 (FGFR4), exhibiting an IC50 value of 5.4 nM. It demonstrates significant antitumor activity by inducing tumor regressions in a xenograft mouse model using the Hep3B2.1-7 hepatocellular carcinoma cell line, while maintaining a favorable toxicity profile. Additionally, FGFR4-IN-6 serves as a click chemistry reagent, featuring an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing compounds, making it a valuable tool for chemical biology applications. -
FGFR1/2/4 Inhibitor
FGFR-IN-16 is a highly potent inhibitor of FGFR1, FGFR2, and FGFR4, exhibiting IC50 values of 8 nM, 4 nM, and 3.8 nM, respectively. This compound is essential for investigating the role of FGFR signaling in various cancers and contributes to the development of targeted therapeutic strategies. Researchers can utilize FGFR-IN-16 to explore the therapeutic potential of FGFR inhibition in diverse malignancies. -
FGFR4 Inhibitor
FGFR4-IN-8 is an ATP-competitive covalent inhibitor targeting fibroblast growth factor receptor 4 (FGFR4). It demonstrates potent activity against both wild-type FGFR4 and its gatekeeper mutants, with IC50 values of 0.5 nM for FGFR4, 0.25 nM for FGFR4V550L, 1.6 nM for FGFR4V550M, and 931 nM for FGFR4C552S. In addition, FGFR4-IN-8 exhibits significant antiproliferative effects on Hep3B hepatocellular carcinoma cells, with an IC50 of 29 nM, and shows modest antitumor efficacy in vivo in the Huh-7 xenograft mouse model, making it a valuable tool for cancer research. -
FGFR2/3 Inhibitor
ISM7594 is an orally active inhibitor targeting FGFR2 and FGFR3. It demonstrates potent antiproliferative activity across various cancer cell lines with alterations in FGFR2 or FGFR3, including amplification, fusion, and mutations, evidenced by IC50 values as low as 0.067 nM in BaF3-TEL-FGFR2-V564F cells. ISM7594 effectively inhibits tumor growth in a dose-dependent manner, making it a valuable tool for investigating advanced solid tumors characterized by FGFR2 or FGFR3 aberrations. -
FGFR3 Inhibitor
FGFR3-IN-3 is a selective inhibitor targeting the Fibroblast Growth Factor Receptor 3 (FGFR3), exhibiting IC50 values of 2.1 nM, 3.1 nM, 4.3 nM, and 74 nM for FGFR1, 2, 3, and 4, respectively. This potent compound demonstrates significant biological activity, making it a valuable tool in the study of bladder cancer and related signaling pathways. Researchers can utilize FGFR3-IN-3 to investigate the therapeutic potential of FGFR inhibition in cancer treatment. -
FGFR Inhibitor
FGFR3-IN-1 is a potent fibroblast growth factor receptor (FGFR) inhibitor, exhibiting IC50 values of 40 nM, 5.1 nM, and 12 nM for FGFR1, FGFR2, and FGFR3, respectively. This compound is particularly relevant for research into bladder cancer, providing valuable insights into FGFR signaling pathways and their role in tumorigenesis. Its selectivity and efficacy make FGFR3-IN-1 a useful tool for investigating therapeutic strategies targeting FGFR-related malignancies. -
PIK3C3/FGFR Inhibitor
MPT0L145 is a selective inhibitor of PIK3C3 and FGFR, demonstrating a Kd value of 0.53 nM for PIK3C3. This compound effectively reduces phosphorylation of FGFR1 and FGFR3, along with their downstream signaling proteins, including FRS2, ERK, and Akt. MPT0L145 induces G0/G1 cell cycle arrest and downregulates cyclin E levels, leading to mitochondrial dysfunction, increased reactive oxygen species production, and DNA damage. As an autophagy inhibitor, MPT0L145 enhances the sensitivity of cancer cells to targeted therapies and chemotherapeutic agents, making it a valuable tool for research in cancer biology, particularly in bladder cancer and non-small cell lung cancer (NSCLC). -
FGFR4 Inhibitor
CXF-007 is a selective inhibitor of fibroblast growth factor receptor 4 (FGFR4) with an IC50 value of 7 nM. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its specificity for FGFR4 positions it as a key reagent for studying FGFR4-mediated signaling pathways and exploring therapeutic options in FGFR4-driven malignancies. -
FGFR1 Inhibitor
FGFR1 inhibitor-14 is a selective inhibitor targeting the Fibroblast Growth Factor Receptor 1 (FGFR1). This compound demonstrates significant anti-proliferative activity in various cancer cell lines, making it a valuable tool in cancer research. It is particularly useful for studies focused on the role of FGFR1 signaling in tumorigenesis and therapeutic response. -
FGFR2/3 Inhibitor
FGFR2/3-IN-2 is a potent inhibitor of FGFR2 and FGFR3, demonstrating IC50 values of 3.7 nM and 31.2 nM, respectively, following a one-hour preincubation. This compound selectively inhibits FGFR2 and FGFR3 without affecting FGFR1/4 or other kinases, minimizing undesirable side effects such as diarrhea and elevated serum phosphate in vivo. FGFR2/3-IN-2 effectively induces tumor stasis or regression in the SNU-16 gastric cancer model, making it a valuable tool for research in cancer biology and targeted therapy. -
FGFR1-3 Inhibitor
AZ8010 is a selective inhibitor targeting fibroblast growth factor receptors 1 to 3 (FGFR1-3). It exhibits significant anti-proliferative activity, making it a valuable tool for cancer research. This compound can be utilized in studies exploring FGFR-related signaling pathways and their implications in tumorigenesis. -
FGFR1 Inhibitor
FGFR1 inhibitor-15 is a selective inhibitor of Fibroblast Growth Factor Receptor 1 (FGFR1), exhibiting an IC50 value of 27 μM. This compound is valuable for cancer research, facilitating the investigation of FGFR1 signaling pathways and their implications in tumor growth and development. Its use can contribute to the understanding of FGFR1-related oncogenic mechanisms and the potential for therapeutic targeting in malignancies. -
FGFR1 Inhibitor
FGFR1 Inhibitor-16 is a selective inhibitor of Fibroblast Growth Factor Receptor 1 (FGFR1). This compound demonstrates an inhibitory efficacy of 53.00% at a concentration of 50 μM and 24.95% at 10 μM. FGFR1 Inhibitor-16 is valuable for research applications focused on cancer, allowing for the exploration of FGFR1 signaling pathways and their roles in tumor biology. -
FGFR1 Inhibitor
FGFR1 inhibitor-17 is a potent inhibitor targeting fibroblast growth factor receptor 1 (FGFR1). This compound demonstrates significant anti-proliferative activity in various cancer models, making it a valuable tool for cancer research. Its ability to inhibit FGFR1 signaling pathways can aid in the investigation of tumor biology and the development of targeted therapies. -
FGFR Inhibitor
SSR128129E free acid is an allosteric inhibitor of fibroblast growth factor receptors (FGFR), exhibiting an IC50 of 1.9 μM for FGFR1. This compound demonstrates significant biological activity in modulating FGFR signaling pathways, making it valuable for research into cancer and other diseases associated with FGFR dysregulation. Its oral availability further facilitates in vivo studies and therapeutic exploration. -
FGFR Inhibitor
FGFR-IN-12 is a selective inhibitor of the Fibroblast Growth Factor Receptor (FGFR). This pyrimidinyl aryl urea derivative exhibits potent inhibition of FGFR activity, making it a valuable tool for investigating pathways involving FGFR signaling. Its efficacy positions FGFR-IN-12 as a significant compound for research applications related to cancer biology and therapeutic development targeting FGFR-related diseases. -
FGFR1/2/3/ CSF-1R Inhibitor
Segigratinib hydrochloride is a selective inhibitor of FGFR1, FGFR2, FGFR3, and CSF-1R, exhibiting IC50 values of 0.5 nM, 1.3 nM, 3.6 nM, and 3.8 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its ability to target multiple receptors involved in tumor progression highlights its potential for therapeutic applications in oncology. -
FGFR4 Inhibitor
FGFR4-IN-7 is a covalent reversible inhibitor of Fibroblast Growth Factor Receptor 4 (FGFR4), exhibiting an IC50 of 0.42 μM. This compound disrupts the FGFR4 signaling pathway, leading to the induction of apoptosis. FGFR4-IN-7 is primarily utilized in research focused on hepatocellular carcinoma (HCC) and offers potential insights into therapeutic strategies targeting this malignancy. -
FGFR/HDAC Inhibitor
HDAC-IN-50 is a potent dual inhibitor targeting FGFR and HDAC with IC50 values of 0.18 nM for FGFR1, 1.2 nM for FGFR2, 0.46 nM for FGFR3, 1.4 nM for FGFR4, and varying inhibitory effects on HDAC isoforms such as HDAC1 (1.3 nM), HDAC2 (1.6 nM), HDAC6 (2.6 nM), and HDAC8 (13 nM). This compound effectively induces apoptosis and causes cell cycle arrest at the G0/G1 phase. Additionally, HDAC-IN-50 decreases the expression of phosphorylated forms of FGFR1, ERK, and STAT3, indicating its potential applications in cancer research and therapy. -
FGFR Inhibitor
FGFR-IN-8 is a potent pan-FGFR inhibitor that targets both wild-type and mutant forms of fibroblast growth factor receptors (FGFRs). With impressive inhibitory potency, it demonstrates IC50 values of less than 0.5 nM against FGFR1, V564F-FGFR2, and FGFR3, alongside 22.6 nM for V555M-FGFR3, and 7.30 nM for FGFR4. This compound induces apoptosis in cancer cells and exhibits notable anticancer properties, making it a valuable reagent for cancer research and therapeutic studies involving FGFR signaling pathways. -
FGFR2 Kinase Inhibitor
Picrasidine Q is a FGFR2 kinase inhibitor derived from the alkaloid components of Angelica keiskei. It exhibits significant anti-cancer properties by inducing apoptosis and causing G1 phase cell cycle arrest in human esophageal cancer cell lines. This compound is valuable for research focused on cancer biology and the molecular mechanisms underlying cell transformation and proliferation. -
VEGFR inhibitor
Brivanib alaninate (BMS-582664) is a dual tyrosine kinase inhibitor of VEGFR and FGFR signaling. -
RTK inhibitor
Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor, which inhibits Ba/F3 cells transformed to IL3 independence by ZNF198-FGFR1 or BCR-FGFR1 with IC50 values of 150 nM and 90 nM, respectively. -
multi-targeted kinase inhibitor
ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively. -
FGFR3 inhibitor
Dovitinib(CHIR-258; TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) with an IC50 of 5 nM. -
tyrosine kinase inhibitor
Sulfatinib (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC50s of in a range of 1 to 24 nM. -
VEGFR-2/FGFR inhibitor
CP-547632 hydrochloride is a well-tolerated, orally-bioavailable inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases with IC50s of 11 nM and 9 nM, respectively. -
FGFR1 inhibitor
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. -
FGFR inhibitor
2,5-Dihydroxybenzoic acid is a derivative of benzoic and a powerful inhibitor of fibroblast growth factors. -
FGFR3 inhibitor
VSPPLTLGQLLS is a small peptide FGFR3 inhibitor, peptide P3, inhibits FGFR3 phosphorylation. VSPPLTLGQLLS inhibits 9-cisRA-induced tracheal lymphangiogenesis and blocks lymphatic endothelial cell (LEC) proliferation, migration, and tubule formation. -
FAK/FGFR2 Inhibitor
PHM16 is an ATP-competitive inhibitor targeting Focal Adhesion Kinase (FAK) and Fibroblast Growth Factor Receptor 2 (FGFR2), with IC50 values of 0.4 μM and 0.37 μM, respectively. This compound exhibits strong anti-angiogenic properties, making it a valuable tool for studies focused on inhibiting tumor angiogenesis and understanding related signaling pathways. Its dual inhibition profile positions PHM16 as an important reagent for cancer research and therapeutic development targeting angiogenesis-related mechanisms. -
Aurora A/B inhibitor
Tinengotinib (TT00420) is an orally bioavailable, 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. It disrupts Aurora kinase-mediated cell cycle progression, inducing G2/M arrest, inhibits the FGFR/JNK-JUN signaling pathway, and activates the MEK/ERK-dependent apoptotic pathway. Tinengotinib exhibits potent anti-tumor proliferation, pro-apoptotic, anti-angiogenic, and tumor microenvironment-modulating activities. It is a promising candidate for research in triple-negative breast cancer (TNBC), gallbladder cancer, and tumor immune microenvironment studies. -
FGFR inhibitor
Gunagratinib (ICP-192) is a low-toxicity, orally active, irreversible pan-FGFR inhibitor that covalently binds to fibroblast growth factor receptors (FGFR1–4), potently and selectively blocking FGFR-mediated signaling. It is designed for the treatment and study of FGFR-driven cancers, including those with FGFR alterations implicated in tumor growth and survival. -
FGFR4 inhibitor
Irpagratinib (ABSK011) is an orally active and highly potent FGFR4 (fibroblast growth factor receptor 4) inhibitor with an IC₅₀ of less than 10 nM. It effectively inhibits FGFR4 autophosphorylation, thereby blocking downstream signaling pathways critical for tumor cell survival and proliferation. Pharmacokinetic studies in mice, rats, and dogs have demonstrated high systemic exposure of Irpagratinib, supporting its potential for oral dosing in clinical applications. In preclinical models, Irpagratinib has shown significant antitumor activity, particularly in subcutaneous xenograft tumor models, making it a promising candidate for the treatment of FGFR4-driven cancers such as hepatocellular carcinoma. -
FGFR inhibitor
Resigratinib (KIN-3248) is an irreversible, orally active covalent inhibitor targeting fibroblast growth factor receptors FGFR1–4. It binds covalently to the conserved cysteine residue Cys492 within the kinase domain, effectively blocking FGFR signaling. Resigratinib demonstrates potent activity against both wild-type FGFRs and clinically relevant drug-resistant mutations, including FGFR2 V565F and FGFR3 V555M. -
FGFR2 inhibitor
Lirafugratinib (RLY-4008) is an orally active, irreversible, and highly selective inhibitor of fibroblast growth factor receptor 2 (FGFR2), with an IC₅₀ of 3 nM. It covalently binds to cysteine 491 (Cys491) in the FGFR2 kinase domain, enabling durable inhibition of FGFR2 signaling. Lirafugratinib is specifically designed to target FGFR2-driven cancers, including those with primary activating alterations and acquired resistance mutations, while sparing other FGFR family members to minimize off-target effects. It has demonstrated potent antitumor activity, including tumor regression, making it a promising therapeutic candidate for FGFR2-altered malignancies such as intrahepatic cholangiocarcinoma and other solid tumors. -
FGFR1 Inhibitor
PD-161570 is a potent ATP-competitive inhibitor of the human fibroblast growth factor receptor 1 (FGFR1) with an IC50 of 39.9 nM and a Ki of 42 nM. It also demonstrates inhibitory effects on platelet-derived growth factor receptor (PDGFR), epidermal growth factor receptor (EGFR), and c-Src tyrosine kinases, with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. Additionally, PD-161570 effectively inhibits PDGF-stimulated autophosphorylation and FGFR phosphorylation, with IC50s of 450 nM and 622 nM, respectively. This compound is relevant in studies of bone morphogenetic proteins (BMPs) and TGF-β signaling pathways.
