Catalog No.
Product Name
Application
Product Information
Citations
-
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). -
VEGFR-2/FGF Inhibitor
CP-547632 TFA is a potent, orally active inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2) and Fibroblast Growth Factor (FGF) kinases, exhibiting IC50 values of 11 nM and 9 nM, respectively. This reagent demonstrates notable selectivity for VEGFR-2 and bFGF over other tyrosine kinases, including EGFR and PDGFRβ. CP-547632 TFA is primarily utilized in cancer research due to its antitumor efficacy, making it a valuable tool for studies focused on angiogenesis and tumor development. -
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. -
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. -
FGFR Inhibitor
FGFR-IN-9 is a potent, reversible inhibitor targeting fibroblast growth factor receptors (FGFRs), demonstrating an IC50 of 17.1 nM against FGFR4WT and varying potency against FGFR1, FGFR2, FGFR3, and FGFR4V550L. This compound is characterized by its oral bioavailability and is primarily utilized in research applications focused on cancer and developmental biology, particularly in elucidating FGFR signaling pathways and their implications in oncogenesis. -
FGFR Modulator
FGFR-IN-3 is a potent modulator of fibroblast growth factor receptors (FGFR) with demonstrated oral bioavailability and blood-brain barrier penetration. This compound exhibits neuroprotective properties, making it a valuable tool in research related to neurodegenerative diseases. FGFR-IN-3's ability to influence FGFR signaling pathways supports its potential in understanding and developing treatments for various neurological conditions. -
VEGFR-2 And FGFR-1 Inhibitor
BMS-645737 is a selective inhibitor of FGF receptor-1 (FGFR-1) and VEGF receptor-2 (VEGFR-2), acting through competitive inhibition of their tyrosine kinase activity. It exhibits potent anti-angiogenic properties, making it a valuable tool in cancer research and studies related to tumor-induced angiogenesis. Additionally, BMS-645737 has been observed to induce lesions in incisor teeth, further highlighting its potential for studying tissue effects and side effects in therapeutic contexts. -
FGFR4 Inhibitor
FGFR4-IN-24 is a selective irreversible inhibitor of FGFR4, exhibiting an IC50 of 1.2 nM. This compound shows minimal activity against other FGFR family kinases (FGFR1-3), allowing for targeted modulation of the FGF19/FGFR4 signaling pathway. FGFR4-IN-24 effectively suppresses the proliferation of the HuH-7 hepatocellular carcinoma cell line with a GI50 of 17 nM and demonstrates significant antitumor efficacy in HuH-7 mouse xenograft models. This reagent is valuable for research applications pertaining to hepatocellular carcinoma. -
FGFR3 Inhibitor
FGFR3-IN-2 is a potent and selective inhibitor of Fibroblast Growth Factor Receptor 3 (FGFR3), exhibiting an IC50 of 4.1 nM against FGFR3, with a significantly higher IC50 of 570 nM for Vascular Endothelial Growth Factor Receptor 2 (VEGFR2). This compound is primarily utilized in research focused on bladder cancer, providing a valuable tool for studying FGFR3-related pathways and potential therapeutic interventions. -
FGFR/CYP Inhibitor
FGFR-IN-10 is an orally bioactive inhibitor targeting fibroblast growth factor receptors (FGFR) and various cytochrome P450 enzymes (CYPs). It demonstrates significant potency against both wild type and V564F mutant FGFR2, with IC50 values of 104.1 nM and 43.6 nM, respectively. Additionally, FGFR-IN-10 inhibits CYP enzymes, including CYP2C9 (IC50: 3.33 µM), CYP2C19 (IC50: 18.75 µM), CYP2D6 (IC50: 4.34 µM), and CYP3A4 (IC50: 0.69 µM). This compound is valuable for researching FGFR-related signaling pathways and the pharmacokinetics of drug metabolism. -
FGFR4 Inhibitor
FGFR4-IN-10 is a potent and selective inhibitor of Fibroblast Growth Factor Receptor 4 (FGFR4), exhibiting an IC50 value of 70.7 nM. This compound demonstrates specificity, showing no inhibition against other members of the FGFR family, including FGFR1, FGFR2, and FGFR3. FGFR4-IN-10 is suitable for research applications focused on cancer biology and therapeutic development targeting FGFR4-mediated signaling pathways. -
FGFR Inhibitor
FGFR-IN-6 is a selective fibroblast growth factor receptor (FGFR) inhibitor. This compound contains an alkyne moiety that enables its use as a click chemistry reagent, facilitating copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. FGFR-IN-6 serves as an essential tool in chemical biology and drug discovery applications, providing insights into FGFR-related signaling pathways and therapeutic interventions. -
FGFR4 Inhibitor
IONIS-FGFR4Rx is an antisense oligonucleotide designed to inhibit fibroblast growth factor receptor 4 (FGFR4), a key player in various signaling pathways associated with renal diseases. This reagent shows potential for research focused on understanding FGFR4's role in pathophysiology and exploring therapeutic strategies in renal disorders. Its specific inhibition of FGFR4 makes it a valuable tool for investigating the molecular mechanisms of kidney disease and developing targeted treatments. -
FGFR2/3 Inhibitor
INCB126503 is a selective inhibitor of FGFR2 and FGFR3, with IC50 values of 2.1 nM and 1.2 nM, respectively. This compound effectively suppresses FGFR signaling in vivo while avoiding hyperphosphatemia, making it suitable for therapeutic applications. INCB126503 demonstrates significant antitumor efficacy in xenograft models that contain FGFR3 genetic alterations, providing valuable insight for research on FGFR-targeted therapies. -
FGFR Inhibitor
FGFR4-IN-17 is a potent FGFR inhibitor, specifically targeting the fibroblast growth factor receptor family. This compound demonstrates inhibition with IC50 values of 24.2 nM for FGFR1, 16.1 nM for FGFR2, 78.0 nM for FGFR3, and 68.0 nM for FGFR4. FGFR4-IN-17 exhibits significant antitumor activity, making it a valuable reagent for cancer research and the study of FGFR-related signaling pathways. -
FGFR Inhibitor
FGFR3-IN-7 is a highly selective inhibitor of the fibroblast growth factor receptor 3 (FGFR3), exhibiting an IC50 value of less than 350 nM. This compound demonstrates significant biological activity in the modulation of FGFR3 signaling pathways, making it a valuable tool for cancer research applications. It is suitable for studies investigating FGFR3's role in tumorigenesis and therapeutic resistance. -
FGFR4 Inhibitor
CXF-009 is a selective and covalent inhibitor of FGFR4, demonstrating an IC50 of 48 nM. By targeting cysteine residues Cys477 and Cys552, CXF-009 effectively modulates FGFR4 activity. This compound is suitable for research applications related to hepatocellular carcinoma, facilitating investigations into FGFR4's role in cancer biology. -
FGFR1 Inhibitor
FGFR1 inhibitor-13 is a selective inhibitor of Fibroblast Growth Factor Receptor 1 (FGFR1), exhibiting an IC50 of 4.2 μM. This compound is primarily utilized in research focusing on cancer biology and angiogenesis, where FGFR1 signaling plays a crucial role. Researchers can leverage FGFR1 inhibitor-13 to investigate the effects of modulating FGFR1 activity in various cellular and in vivo models. -
FGFR3 Inhibitor
FGFR3-IN-9 is a selective inhibitor of Fibroblast Growth Factor Receptor 3 (FGFR3), which plays a crucial role in various cellular processes including proliferation and differentiation. This compound is primarily used in research focused on cancer biology, particularly in models of FGFR3-driven malignancies. Its potent inhibitory activity makes it a valuable tool for studying FGFR3 signaling pathways and exploring targeted therapeutic strategies. -
FGFR2/3 Inhibitor
FGFR2/3-IN-1 is a selective inhibitor targeting FGFR2 and FGFR3, exhibiting IC50 values of 1 nM and 0.5 nM, respectively. This compound demonstrates over 40-fold selectivity against FGFR1 and FGFR4, as well as across the wider kinome. Additionally, FGFR2/3-IN-1 effectively inhibits FGFR3 mutants V555L and V555M, with IC50s of 2.7 nM and 6.1 nM, respectively. It is primarily used in research applications focused on cancer biology and receptor signaling pathways. -
FGFR2/3 Inhibitor
FGFR2/3-IN-3 is a potent dual inhibitor of Fibroblast Growth Factor Receptors 2 and 3 (FGFR2/3), demonstrating IC50 values of 2.7 nM and 3.9 nM, respectively, against TEL-FGFR2 and TEL-FGFR3. It effectively targets both wild-type and mutant FGFR3, with minimal impact on CYP3A4 and hERG functions. FGFR2/3-IN-3 enhances the balance of chondrocyte proliferation and differentiation, promoting bone growth by blocking the signaling mediated by mutant FGFR3. This compound shows promise in animal models of dwarfism and may contribute to research on bone development disorders, including achondroplasia (ACH). -
FGFR4 Inhibitor
FGFR4-IN-13 is a selective inhibitor of fibroblast growth factor receptor 4 (FGFR4), primarily involved in the regulation of cellular proliferation and survival pathways. This compound demonstrates notable anti-tumor activity, making it a valuable tool for investigating hepatocellular carcinoma. FGFR4-IN-13 facilitates research aimed at understanding the molecular underpinnings of this cancer type and developing targeted therapeutic strategies. -
FGFR Modulator
SUN13837 is a potent orally active modulator of fibroblast growth factor receptors (FGFRs) with the ability to penetrate the blood-brain barrier. It exhibits neuroprotective properties, making it relevant for research in neurodegenerative diseases. This compound can serve as a valuable tool for investigating therapeutic interventions in FGFR-related neurological conditions. -
FGFR-4 Inhibitor
FGFR4-IN-16 is a selective covalent inhibitor targeting the fibroblast growth factor receptor 4 (FGFR-4). It demonstrates potent activity in disrupting FGFR-4 signaling pathways, making it relevant for cancer research. This compound may be utilized in studies investigating the role of FGFR-4 in tumor growth and progression, providing valuable insights into therapeutic strategies for FGFR-4-dependent malignancies. -
FGFR Inhibitor
FGFR-IN-5 is a selective inhibitor of fibroblast growth factor receptor (FGFR), a critical tyrosine kinase receptor implicated in various cancer pathways. This compound demonstrates significant biological activity in inhibiting FGFR signaling, making it valuable for cancer research applications. Additionally, FGFR-IN-5 possesses an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), thus serving as a versatile click chemistry reagent for further molecular investigations. -
FGFR Inhibitor
FGFR-IN-11 is a potent covalent inhibitor of Fibroblast Growth Factor Receptors (FGFR), demonstrating IC50 values of 9.9 nM for FGFR1, 3.1 nM for FGFR2, 16 nM for FGFR3, and 1.8 nM for FGFR4. This compound effectively hinders the proliferation of various cancer cell lines at nanomolar concentrations and significantly reduces tumor growth in xenograft mouse models. FGFR-IN-11 serves as a valuable tool for research into targeted cancer therapies and the underlying mechanisms of FGFR-mediated tumorigenesis. -
FGFR4 Inhibitor
FGFR4-IN-12 is a selective inhibitor targeting Fibroblast Growth Factor Receptor 4 (FGFR4), demonstrating enhanced potency and specificity. This compound exhibits significant anti-proliferative effects against FGFR4-dependent hepatocellular carcinoma (HCC) cell lines, making it valuable for cancer research. Additionally, FGFR4-IN-12 features an alkyne functional group, enabling its use as a click chemistry reagent that can participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
FGFR Inhibitor
FGFR-IN-13 is an irreversible covalent inhibitor of fibroblast growth factor receptors (FGFR), specifically targeting FGFR1 (IC50 = 0.20 ± 0.02 nM) and FGFR4 (IC50 = 0.40 ± 0.03 nM). This compound modulates FGFR-mediated signaling pathways by downregulating total PARP and Bcl-2 protein levels while promoting the expression of Cleaved-PARP and Bax in a dose-dependent manner. FGFR-IN-13 exhibits significant antitumor activity, making it a valuable tool for cancer research and therapeutic applications involving FGFR signaling pathways.
