Catalog No.
Product Name
Application
Product Information
Citations
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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. -
PROTAC FGFR2 Degrader
LC-MB12 is an orally active PROTAC compound that targets FGFR2 degradation, with a DC₅₀ of 11.8 nM. It consists of the FGFR2 inhibitor BGJ398, a PROTAC linker, and a cereblon (CRBN) ligand. LC-MB12 effectively inhibits FGFR2 signaling in gastric cancer cells and exhibits antitumor activity. -
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. -
FGFR2 Degrader
PROTAC FGFR2 degrader 1 is a specialized degrader designed to selectively target and degrade FGFR2, exhibiting a DC50 of 6.46 nM and an FGFR2 IC50 of 0.08 nM. This compound demonstrates significant anti-proliferative activity, inducing G0/G1 cell cycle arrest in KATOIII and SNU16 cell lines while inhibiting apoptosis through modulation of downstream signaling proteins, p-ERK and p-PLCγ. In in vivo studies, PROTAC FGFR2 degrader 1 effectively suppresses the growth of SNU16 xenograft tumors, showcasing its potential for research in gastric cancer therapeutic applications. -
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. -
FGFR2 ADC
Aprutumab ixadotin is an antibody-drug conjugate (ADC) that targets fibroblast growth factor receptor 2 (FGFR2). It combines a fully human anti-FGFR2 monoclonal antibody with an innovative non-cleavable linker conjugated to an Auristatin W derivative. This reagent is primarily utilized in research focused on advanced solid tumors, including FGFR2-positive gastric cancer and triple-negative breast cancer, facilitating the exploration of targeted therapies in these malignancies. -
FGFR1 Agonist
TCB-32 is a potent FGFR1 agonist with an EC50 of 0.88 μM, effectively activating the FGFR1 signaling pathway to enhance cell proliferation, notably through the ERK 1/2 cascade. This compound exhibits excellent thermal stability and can serve as a substitute for bFGF in serum-free cell culture environments. TCB-32 is applicable in research related to tissue repair and wound healing, making it suitable for studies investigating conditions such as psoriasis and eczema. -
FGFR3/BRAF Binder
2,4,3',4',6'-Penta-O-(3-methylbutanoyl)sucrose functions as a selective binder for Fibroblast Growth Factor Receptor 3 (FGFR3) and BRAF, playing a pivotal role in modulating pathways associated with cancer progression. Derived from Atractylodes japonica, this compound exhibits low cytotoxicity towards cancer cell lines, making it a suitable candidate for research applications focused on targeted cancer therapies and signaling pathway studies. Its unique structural characteristics enhance its potential for further exploration in drug development and therapeutic interventions. -
bFGF/FGFR1 Ligand
bFGF (119-126) is a peptide ligand that selectively targets FGFR1, disrupting the bFGF-FGFR1 interaction, which leads to inhibition of FGFR1 phosphorylation and subsequent downstream signaling pathways. This results in the promotion of apoptosis and suppression of cell proliferation, migration, angiogenesis, and metastasis. Additionally, when conjugated with a carrier, bFGF (119-126) enhances cellular uptake through FGFR-mediated endocytosis, serving as an effective FGFR-targeting agent. Its applications extend to research in various cancers, including lung cancer, breast cancer, glioblastoma, and ovarian cancer, particularly when combined with ultrasound and Doxorubicin to potentiate antitumor effects. -
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. -
FGFR-β-klotho complex Activator
Efimosfermin alfa is a genetically modified variant of FGF21 that activates the FGFR1c/β-Klotho complex. This compound plays a critical role in metabolic regulation, specifically in the context of metabolic dysfunction-associated steatohepatitis, obesity, and mild hypertriglyceridemia. Its unique mechanism of action makes it a valuable tool for research exploring metabolic disorders and their associated pathways. -
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. -
FGFR3-TACC3 Degrader
SNIPER(TACC3)-11 is a potent degrader of the FGFR3-TACC3 fusion protein, utilizing targeted protein degradation to reduce its levels within cells. This compound effectively suppresses the proliferation of cancer cells that express the FGFR3-TACC3 fusion, making it a valuable tool for research related to targeting oncogenic protein fusions in cancer therapy. Its potential applications include studies in cancer biology and the development of novel therapeutic strategies against FGFR3-TACC3-positive tumors. -
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. -
PROTAC FGFR1/2 Degrader
DGY-09-192 is a PROTAC degrader targeting FGFR1 and FGFR2, demonstrating DC50 values of 4.35 nM and 70 nM, respectively. This compound selectively degrades both wild-type FGFR1/2 and various FGFR2 fusion proteins, such as FGFR2-PHGDH and FGFR2-OPTN. By suppressing downstream FGFR signaling, DGY-09-192 effectively reduces the phosphorylation of key targets including FRS2 Y196 and ERK1/2 T202/Y204, making it a valuable tool for investigating FGFR-driven malignancies in both in vitro and in vivo studies. -
FGFR Activator
FGL peptide is a fibroblast growth factor receptor (FGFR) activator that effectively penetrates the blood-brain barrier. It initiates NCAM-FGFR and FGFR1 signaling pathways, which modulate the expression of genes involved in apoptosis, signal transduction, and metabolic regulation. FGL peptide is primarily utilized in research focused on traumatic brain injury, offering insights into its underlying molecular mechanisms and potential therapeutic targets. -
FGFR1 Agonist
TCB-32 hydrochloride is an FGFR1 agonist with an EC50 of 0.88 μM. This compound effectively enhances cell proliferation by activating the FGFR1 signaling pathway, notably promoting downstream ERK 1/2 activity. With excellent thermal stability, TCB-32 hydrochloride serves as a viable replacement for bFGF in serum-free cell culture media. Its applications extend to tissue repair and the study of wound healing in diseases such as psoriasis and eczema. -
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). -
Recombinant FGFR3
Recifercept is a soluble recombinant fibroblast growth factor receptor 3 (FGFR3) designed to act as a decoy or ligand trap. By binding to fibroblast growth factors, it reduces their availability to mutant FGFR3 receptors, thereby modulating their activity. This reagent is particularly valuable for research focused on achondroplasia and related conditions involving FGFR3 mutations. -
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.
