FGFR

Cat. No.

A33504

CAS No.

2226238-09-9

Recifercept

Synonyms: TA-46; sFGFR3

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.

Cat. No.

A33505

CAS No.

1513860-41-7

FGFR-IN-1

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.

Cat. No.

A33510

CAS No.

1265966-31-1

S49076 hydrochloride

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.

Cat. No.

A33511

CAS No.

2388506-51-0

MAX-40279 hydrochloride

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.

Cat. No.

A33512

CAS No.

2388506-43-0

MAX-40279 hemifumarate

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.

Cat. No.

A33513

CAS No.

1879965-80-6

E7090 succinate

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.

Cat. No.

A33514

CAS No.

2396664-85-8

FGFR4-IN-11

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.

Cat. No.

A33515

CAS No.

2230973-67-6

FGFR4-IN-4

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.

Cat. No.

A33516

CAS No.

2093088-81-2

FIIN-4

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.

Cat. No.

A33517

CAS No.

3027827-02-4

FGFR4-IN-14

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).

Cat. No.

A33518

CAS No.

2410612-08-5

FGFR1 inhibitor-2

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.

Cat. No.

A33519

CAS No.

2761211-49-6

FGFR-IN-4

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.

Cat. No.

A33520

CAS No.

1314021-57-2

ARQ 069

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.

Cat. No.

A33521

CAS No.

1628537-44-9

Fanregratinib

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.

Cat. No.

A33522

CAS No.

2922812-74-4

FGFR4-IN-22

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.

Cat. No.

A33524

CAS No.

2833703-72-1

FGFR3-IN-6

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.

Cat. No.

A33525

CAS No.

2665665-09-6

FGFR-IN-2

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.

Cat. No.

A33527

CAS No.

2833706-13-9

FGFR3-IN-4

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.

Cat. No.

A33528

CAS No.

3024090-08-9

FGFR-IN-9

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.

Cat. No.

A33529

CAS No.

2488762-63-4

FGFR-IN-3

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.

Cat. No.

A33530

CAS No.

651744-16-0

BMS-645737

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.

Cat. No.

A33531

CAS No.

3053546-73-6

FGFR4-IN-24

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.

Cat. No.

A33533

CAS No.

2428742-58-7

FGFR3-IN-2

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.

Cat. No.

A33536

CAS No.

2847092-41-3

FGFR-IN-10

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.

Cat. No.

A33538

CAS No.

2857862-25-8

FGFR4-IN-10

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.