FGFR

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.

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.

Cat. No.

A33539

CAS No.

2762955-18-8

FGFR-IN-6

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.

Cat. No.

A33541

CAS No.

1416376-17-4

IONIS-FGFR4Rx

Synonyms: ISIS 463588

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.

Cat. No.

A33542

CAS No.

2640089-88-7

INCB126503

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.

Cat. No.

A33543

CAS No.

3011805-61-8

FGFR4-IN-17

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.

Cat. No.

A33544

CAS No.

2833703-79-8

FGFR3-IN-7

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.

Cat. No.

A33545

CAS No.

2727084-00-4

CXF-009

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.

Cat. No.

A33546

CAS No.

670266-26-9

FGFR1 inhibitor-13

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.

Cat. No.

A33547

CAS No.

2446523-17-5

FGFR3-IN-9

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.

Cat. No.

A33548

CAS No.

2640352-86-7

FGFR2/3-IN-1

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.

Cat. No.

A33549

CAS No.

3069945-78-1

FGFR2/3-IN-3

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).

Cat. No.

A33550

CAS No.

2020395-38-2

FGFR4-IN-13

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.

Cat. No.

A33552

CAS No.

1970120-44-5

FGFR4-IN-16

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.

Cat. No.

A33553

CAS No.

2762750-70-7

FGFR-IN-5

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.

Cat. No.

A33554

CAS No.

2658488-68-5

FGFR-IN-11

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.

Cat. No.

A33557

CAS No.

2423992-63-4

FGFR4-IN-12

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.