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Catalog No.
Product Name
Application
Product Information
Citations
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FLT3 Inhibitor
JI6 is a potent and selective FLT3 inhibitor, exhibiting IC50 values of approximately 40 nM for FLT3-WT, 8 nM for FLT3-D835Y, and 4 nM for FLT3-D835H. Additionally, JI6 demonstrates inhibitory activity against JAK3 and c-Kit, with IC50 values of around 250 nM and 500 nM, respectively. This compound serves as a valuable tool for research applications focused on acute myeloid leukemia. -
BET/JAK2/FLT3 Inhibitor
SG3-179 is a selective inhibitor of BET bromodomain proteins, with additional activity against JAK2 and FLT3. This compound effectively reduces HOXB13 protein expression, demonstrating potential relevance in the study of multiple myeloma (MM1.S). SG3-179 is a valuable tool for research involving epigenetic regulation and signaling pathways associated with hematological malignancies. -
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. -
PDGFR Inhibitor
(Z)-Orantinib is a selective, orally active ATP-competitive inhibitor targeting PDGFRβ, as well as Flk‐1/KDR and FGFR1, with IC50 values of 0.008 µM, 2.1 µM, and 1.2 µM, respectively. This compound exhibits significant antiangiogenic and antitumor properties, effectively inducing regression of established tumors. It is a valuable tool for research applications focused on cancer biology and the mechanisms of angiogenesis. -
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. -
VEGFR2 Inhibitor
JK-P3 is a selective inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) with IC50 values of 7.83 μM for VEGFR2, 27 μM for FGFR1, and 5.18 μM for FGFR3. It effectively blocks VEGF-A-induced VEGFR2 activation and downstream signaling pathways, demonstrating inhibition of endothelial cell migration and angiogenesis in vitro. Additionally, JK-P3 suppresses fibroblast growth factor receptor kinase activity, contributing to its anti-angiogenic properties and making it a valuable tool for research in vascular biology and cancer therapeutics. -
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). -
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. -
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. -
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.
