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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
FGFR3 Inhibitor
Dabogratinib is a selective inhibitor of FGFR3, displaying an IC50 of 11 nM. It demonstrates significant antitumor activity against urothelial carcinoma and various solid tumors by downregulating FGFR3 and ERK1/2 signaling pathways, leading to tumor growth inhibition and regression in FGFR3-altered xenograft models. Additionally, Dabogratinib enhances chondrocyte proliferation and differentiation, promotes endochondral bone formation, and improves craniofacial and spinal morphology. This compound is valuable for research into metastatic urothelial carcinoma, achondroplasia, and hypochondroplasia. -
FGFR2 Inhibitor
FGFR2-IN-2 is a selective inhibitor of fibroblast growth factor receptor 2 (FGFR2), demonstrating inhibitory potency with an IC50 value of 29 nM against FGFR2, and 389 nM and 758 nM for FGFR1 and FGFR3, respectively. This compound exhibits potential in the study of FGFR-related signaling pathways and can be utilized in research focused on cancer therapeutics, particularly in tumors with aberrant FGFR2 activity. -
FGFR Inhibitor
FIIN-1 is a selective, irreversible inhibitor of fibroblast growth factor receptors (FGFR1, FGFR2, FGFR3, and FGFR4). It exhibits potent binding affinity, with Kd values of 2.8 nM for FGFR1, 6.9 nM for FGFR2, 5.4 nM for FGFR3, and 120 nM for FGFR4, alongside Kd values of 32 nM and 120 nM for Flt1 and Flt4, respectively. With biochemical IC50 values of 9.2 nM for FGFR1, 6.2 nM for FGFR2, 11.9 nM for FGFR3, and 189 nM for FGFR4, FIIN-1 is valuable for research applications focused on FGFR-related pathways in cancer and developmental biology. -
FGFR1 Inhibitor
FGFR1 inhibitor-10 is a potent FGFR1 inhibitor with an IC50 value of 28 nM. It effectively inhibits the phosphorylation of FGFR1, leading to significant anti-angiogenic, anti-invasive, and anti-tumor activities. This compound is valuable for research applications focused on understanding FGFR1 signaling pathways and developing therapies for cancers characterized by aberrant FGFR1 activity. -
FGFR3 Inhibitor
FGFR3-IN-5 is a potent and selective inhibitor of Fibroblast Growth Factor Receptor 3 (FGFR3), exhibiting IC50 values of 3 nM for FGFR3, 44 nM for FGFR2, and 289 nM for FGFR1. This compound demonstrates effective inhibition of FGFR3 signaling pathways, making it a valuable tool for cancer research. FGFR3-IN-5 is suitable for studies investigating the role of FGFR3 in tumorigenesis and therapeutic response. -
FLT3/FGFR Inhibitor
MAX-40279 is a dual inhibitor targeting FLT3 and FGFR kinases, exhibiting potent activity against both wild-type and FLT3 mutants, including FLT3D835Y. This compound effectively inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 is valuable for research applications in acute myelogenous leukemia (AML), particularly in studying resistance mechanisms to existing therapies. -
FGFR (1-3) Inhibitor
CPL304110 is a selective inhibitor of fibroblast growth factor receptors FGFR1-3, demonstrating potent activity with IC50 values of 0.75 nM, 0.5 nM, and 3.05 nM for each receptor, respectively. This orally active compound is valuable in research applications aimed at understanding FGFR signaling pathways and their role in various cancers and pathological conditions. Its efficacy in modulating FGFR activity makes it a valuable tool for investigating therapeutic strategies targeting fibroblast growth factor receptor-mediated processes. -
FGFR2 Inhibitor
Lirafugratinib hydrochloride is an orally active, irreversible inhibitor specifically targeting FGFR2 with an IC50 of 3 nM. It covalently binds to the cysteine residue Cys491, effectively addressing FGFR2 primary alterations and resistance mutations. This compound is designed to induce tumor regression while exhibiting minimal impact on other FGFR family members, making it valuable for research in cancer therapeutics focused on FGFR-dependent malignancies. -
FGFR Inhibitor
FGFR2-IN-1 is a selective inhibitor of Fibroblast Growth Factor Receptor 2 (FGFR2), exhibiting an IC50 of 140 nM. This compound effectively modulates FGFR2 activity, demonstrating significant biological activity relevant to cancer research. It is utilized in various studies focusing on tumorigenesis and the role of FGFR signaling pathways in malignancies. -
FGFR4 Inhibitor
FGFR4-IN-5 is a selective covalent inhibitor of fibroblast growth factor receptor 4 (FGFR4) with an IC50 of 6.5 nM. It demonstrates significant anti-tumor activity in vivo, making it a valuable tool for research focused on hepatocellular carcinoma. This compound is ideal for studies investigating FGFR4-mediated signaling pathways and therapeutic strategies in cancer treatment. -
FGFR1 Inhibitor
CYY292 is an FGFR1 inhibitor that targets the FGFR1/AKT/Snail signaling pathway, demonstrating significant effects in glioblastoma (GBM) cells. This compound effectively inhibits cancer cell proliferation and reduces epithelial-mesenchymal transition, stemness, invasion, and migration in a dose-dependent manner. CYY292 is a valuable reagent for research applications aimed at understanding the molecular underpinnings of GBM and exploring potential therapeutic strategies. -
FGFR2 Inhibitor
FGFR2-IN-3 is a selective inhibitor of fibroblast growth factor receptor 2 (FGFR2). It exhibits strong binding affinity, facilitating critical interactions and inducing conformational alterations in the receptor. This compound is primarily utilized in cancer research, particularly in investigations focused on tumor biology and signaling pathways involving FGFR2. -
VEGFR/FGFR Inhibitor
Lucitanib dihydrochloride is a selective dual inhibitor targeting VEGFR and FGFR, demonstrating potent inhibition of VEGFR1, VEGFR2, VEGFR3, FGFR1, and FGFR2 with IC50 values of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively. This inhibitor plays a critical role in regulating angiogenesis and tumor growth, making it valuable for research in cancer biology and therapeutic development. Lucitanib dihydrochloride is suitable for studies focused on vascular endothelial growth factor signaling pathways and fibroblast growth factor signaling, contributing to the understanding of tumor microenvironment interactions. -
FGFR1/2/3 Inhibitor
TYRA-200 is an orally active inhibitor of FGFR1, FGFR2, and FGFR3. This compound demonstrates dose-dependent tumor regression in mice models expressing both wild-type and mutant FGFR2. TYRA-200 serves as a valuable tool for investigating advanced or metastatic intrahepatic cholangiocarcinoma and other solid tumors driven by FGFR2 mutations in preclinical research. -
FGFR Inhibitor
Derazantinib Racemate is an ATP-competitive inhibitor targeting fibroblast growth factor receptors (FGFR1-3). This compound demonstrates potent inhibitory activity in chondrocytes, with IC50 values of 4.5 nM for FGFR1, 1.8 nM for FGFR2, and 4.5 nM for FGFR3. It is suitable for research applications focused on FGFR-related signaling pathways and their implications in various cancers and diseases. -
FLT3/FGFR Inhibitor
MAX-40279 hemiadipate is a dual inhibitor of FLT3 and FGFR kinases, exhibiting oral bioactivity. This compound effectively targets multiple FLT3 mutants, including FLT3D835Y, and has the potential to overcome resistance against existing treatments. Inhibition of NDRG1 phosphorylation at Ser330 and suppression of endothelial-to-mesenchymal transition (EndMT) further characterize its biological activity. MAX-40279 hemiadipate is a valuable tool for research into acute myelogenous leukemia (AML). -
FGFR Inhibitor
FGFR-IN-1 is a highly potent inhibitor of fibroblast growth factor receptors (FGFR1, FGFR2, and FGFR3), with an IC50 of less than 100 nM for each receptor. This compound effectively disrupts FGFR-mediated signaling pathways, making it a valuable tool for research into cancer biology and angiogenesis. Its specific inhibition profile supports investigations into the role of FGFRs in various pathophysiological conditions and aids in the development of targeted therapies. -
FGFR Inhibitor
S49076 hydrochloride is a potent inhibitor targeting FGFR1, FGFR2, FGFR3, MET, and AXL/MER. With IC50 values below 20 nM, it demonstrates significant biological activity in inhibiting these receptor tyrosine kinases. This compound is primarily used in research applications focusing on cancer biology, particularly in studies involving tumor growth and angiogenesis mediated by FGFR signaling pathways. -
FLT3/FGFR Inhibitor
MAX-40279 hydrochloride is a dual inhibitor targeting FLT3 and FGFR kinases. This compound demonstrates efficacy against FLT3 mutants, including FLT3D835Y, potentially overcoming resistance to existing therapies. MAX-40279 hydrochloride has been shown to inhibit NDRG1 phosphorylation at Ser330 and suppress endothelial-to-mesenchymal transition (EndMT). It is suited for research focused on acute myelogenous leukemia (AML) and related pathways. -
FLT3/FGFR Inhibitor
MAX-40279 hemifumarate is an orally active dual inhibitor of FLT3 and FGFR kinases, demonstrating efficacy against FLT3 mutant variants, including FLT3D835Y. This compound effectively inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 hemifumarate is relevant for research in acute myelogenous leukemia (AML) and offers potential therapeutic insights into overcoming resistance associated with traditional FLT3 inhibitors. -
FGFR1/2/3 Inhibitor
E7090 succinate is a selective and potent inhibitor targeting FGFR1, FGFR2, and FGFR3, exhibiting IC50 values of 0.71 nM, 0.50 nM, and 1.2 nM, respectively. This orally bioavailable compound disrupts FGFR-mediated signaling pathways, making it valuable for research in cancer biology and therapeutic development. Its inhibition profiles support investigations into diseases characterized by aberrant FGFR activity. -
FGFR4 Inhibitor
FGFR4-IN-11 is a potent, selective covalent inhibitor of FGFR4 with an IC50 of 2.1 nM. This compound effectively disrupts the FGF19/FGFR4 signaling pathway, demonstrating significant antitumor activity. FGFR4-IN-11 is valuable for research applications focused on cancer biology and the therapeutic potential of targeting fibroblast growth factor receptors. -
FGFR4 Inhibitor
FGFR4-IN-4 is a potent FGFR4 inhibitor designed to interfere with Fibroblast Growth Factor Receptor 4 signaling. This compound exhibits significant anti-tumor activity, making it a valuable tool for cancer research. It is relevant for studies focusing on targeting FGFR4-related pathways and developing therapeutic strategies against FGFR4-driven malignancies. -
FGFR Inhibitor
FIIN-4 is a first-in-class, orally active covalent inhibitor targeting fibroblast growth factor receptors (FGFRs). It exhibits potent inhibitory activity, displaying IC50 values of 2.6 nM for FGFR1 and FGFR2, 5.6 nM for FGFR3, and 9.2 nM for FGFR4. FIIN-4 is utilized in research to investigate its efficacy in inhibiting metastatic tumor growth, making it a valuable tool in cancer biology studies. -
FGFR4 Inhibitor
FGFR4-IN-14 is a selective inhibitor of Fibroblast Growth Factor Receptor 4 (FGFR4) with an IC50 of 2.4 nM. It demonstrates significant antitumor activity by inhibiting the proliferation of V550L and N535K mutant strains, exhibiting IC50 values of 21 nM and 2.5 nM against BaF3/ETV6-FGFR4-V550L and BaF3/ETV6-FGFR4-N535K cells, respectively. Additionally, FGFR4-IN-14 has shown promising efficacy in the Huh7 xenograft model, making it a valuable tool for research in hepatocellular carcinoma (HCC). -
FGFR1 Inhibitor
FGFR1 inhibitor-2 is a selective inhibitor of the fibroblast growth factor receptor 1 (FGFR1), with an IC50 of 4.55 μM in MDA-MB-231 human breast cancer cells. This compound demonstrates significant anti-proliferative activity and is primarily utilized in research focused on metastatic triple-negative breast cancer, enabling investigations into signaling pathways and therapeutic strategies targeting FGFR1. -
FGFR Inhibitor
FGFR-IN-4 is a potent fibroblast growth factor receptor (FGFR) inhibitor, targeting the tyrosine kinase activity associated with FGFR activation. This compound is significant for research into cancer biology, enabling studies on FGFR-related signaling pathways and tumor progression. Additionally, FGFR-IN-4 features an alkyne group, making it suitable for applications in click chemistry, specifically facilitating copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
FGFR Inhibitor
ARQ 069 is a potent FGFR inhibitor that selectively targets the unphosphorylated, inactive forms of FGFR1 and FGFR2 kinases, demonstrating IC50 values of 0.84 μM and 1.23 μM, respectively. This compound effectively inhibits FGFR1 and FGFR2 autophosphorylation with IC50 values of 2.8 μM and 1.9 μM, respectively, through a non-ATP competitive mechanism. ARQ 069 is suitable for research applications investigating FGFR-related signaling pathways and their implications in various cancers. -
FGFR Tyrosine Kinase Inhibitor
Fanregratinib is an FGFR tyrosine kinase inhibitor that selectively targets fibroblast growth factor receptors. It is known for its ability to impede cancer cell proliferation and survival by disrupting downstream signaling pathways associated with FGFR activation. This compound is primarily used in research related to cancer therapeutics and the study of FGFR-mediated pathways. Its application extends to investigating the role of FGFR in various malignancies, providing insights for potential treatment strategies. -
FGFR4 Inhibitor
FGFR4-IN-22 is a selective inhibitor of Fibroblast Growth Factor Receptor 4 (FGFR4), exhibiting a potent inhibitory activity with an IC50 value of 5.4 nM. This compound serves as a promising lead for the development of anti-hepatocellular carcinoma (HCC) agents, making it relevant for cancer research and therapeutic investigations targeting FGFR4 signaling pathways. Its application in preclinical studies could facilitate the exploration of FGFR4 as a viable therapeutic target in other malignancies as well. -
FGFR Inhibitor
FGFR3-IN-6 is a selective inhibitor of Fibroblast Growth Factor Receptor 3 (FGFR3), exhibiting an IC50 value of less than 350 nM. This compound effectively inhibits FGFR3 activity, making it a valuable tool for investigating FGFR3-mediated signaling pathways in cancer research. Its specificity and potency facilitate studies on tumorigenesis and therapeutic strategies targeting FGFR3-related malignancies. -
FGFR Inhibitor
FGFR-IN-2 is a selective fibroblast growth factor receptor (FGFR) inhibitor that exhibits potent inhibitory activity with IC50 values of 7.3 nM, 4.3 nM, 7.6 nM, and 11 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. Its strong affinity for FGFRs positions FGFR-IN-2 as a valuable tool for cancer research, particularly in studies targeting FGFR-related signaling pathways and tumor progression. -
FGFR3 Inhibitor
FGFR3-IN-4 is a selective inhibitor of Fibroblast Growth Factor Receptor 3 (FGFR3), demonstrating an IC50 value of less than 50 nM. This compound exhibits over tenfold selectivity for FGFR3 compared to FGFR1, making it a valuable tool for studying FGFR3-mediated pathways. FGFR3-IN-4 is applicable in research focused on cancer therapeutics and skeletal disorders, where aberrant FGFR3 signaling is implicated.
