FGFR

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.

A33551

CAS No.

1080650-67-4

SUN13837

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.

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.

Cat. No.

A33558

CAS No.

2962941-25-7

FGFR-IN-13

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.

Cat. No.

A33559

CAS No.

1431872-18-2

FGFR-IN-22

FGFR-IN-22 is a potent FGFR inhibitor, demonstrating IC50 values of 0.631 nM for FGFR1, 1.26 nM for FGFR2, 0.851 nM for FGFR3, and 1 nM for FGFR4. This compound effectively inhibits cell proliferation linked to FGFR1 and FGFR3 signaling pathways, making it a valuable tool for research in cancer types such as chronic lymphocytic leukemia (CLL). FGFR-IN-22 is useful for studying the role of FGFRs in tumor biology and therapeutic development.

Cat. No.

A33560

CAS No.

2760970-10-1

FGFR4-IN-6

FGFR4-IN-6 is a covalent, reversible inhibitor of Fibroblast Growth Factor Receptor 4 (FGFR4), exhibiting an IC50 value of 5.4 nM. It demonstrates significant antitumor activity by inducing tumor regressions in a xenograft mouse model using the Hep3B2.1-7 hepatocellular carcinoma cell line, while maintaining a favorable toxicity profile. Additionally, FGFR4-IN-6 serves as a click chemistry reagent, featuring an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing compounds, making it a valuable tool for chemical biology applications.

Cat. No.

A33565

CAS No.

2170748-42-0

FGFR-IN-16

FGFR-IN-16 is a highly potent inhibitor of FGFR1, FGFR2, and FGFR4, exhibiting IC50 values of 8 nM, 4 nM, and 3.8 nM, respectively. This compound is essential for investigating the role of FGFR signaling in various cancers and contributes to the development of targeted therapeutic strategies. Researchers can utilize FGFR-IN-16 to explore the therapeutic potential of FGFR inhibition in diverse malignancies.

Cat. No.

A33566

CAS No.

2765240-52-4

FGFR4-IN-8

FGFR4-IN-8 is an ATP-competitive covalent inhibitor targeting fibroblast growth factor receptor 4 (FGFR4). It demonstrates potent activity against both wild-type FGFR4 and its gatekeeper mutants, with IC50 values of 0.5 nM for FGFR4, 0.25 nM for FGFR4V550L, 1.6 nM for FGFR4V550M, and 931 nM for FGFR4C552S. In addition, FGFR4-IN-8 exhibits significant antiproliferative effects on Hep3B hepatocellular carcinoma cells, with an IC50 of 29 nM, and shows modest antitumor efficacy in vivo in the Huh-7 xenograft mouse model, making it a valuable tool for cancer research.

Cat. No.

A33567

CAS No.

3025799-76-9

ISM7594

ISM7594 is an orally active inhibitor targeting FGFR2 and FGFR3. It demonstrates potent antiproliferative activity across various cancer cell lines with alterations in FGFR2 or FGFR3, including amplification, fusion, and mutations, evidenced by IC50 values as low as 0.067 nM in BaF3-TEL-FGFR2-V564F cells. ISM7594 effectively inhibits tumor growth in a dose-dependent manner, making it a valuable tool for investigating advanced solid tumors characterized by FGFR2 or FGFR3 aberrations.

Cat. No.

A33568

CAS No.

2428738-41-2

FGFR3-IN-3

FGFR3-IN-3 is a selective inhibitor targeting the Fibroblast Growth Factor Receptor 3 (FGFR3), exhibiting IC50 values of 2.1 nM, 3.1 nM, 4.3 nM, and 74 nM for FGFR1, 2, 3, and 4, respectively. This potent compound demonstrates significant biological activity, making it a valuable tool in the study of bladder cancer and related signaling pathways. Researchers can utilize FGFR3-IN-3 to investigate the therapeutic potential of FGFR inhibition in cancer treatment.

Cat. No.

A33570

CAS No.

2428743-04-6

FGFR3-IN-1

FGFR3-IN-1 is a potent fibroblast growth factor receptor (FGFR) inhibitor, exhibiting IC50 values of 40 nM, 5.1 nM, and 12 nM for FGFR1, FGFR2, and FGFR3, respectively. This compound is particularly relevant for research into bladder cancer, providing valuable insights into FGFR signaling pathways and their role in tumorigenesis. Its selectivity and efficacy make FGFR3-IN-1 a useful tool for investigating therapeutic strategies targeting FGFR-related malignancies.

Cat. No.

A33571

CAS No.

2070837-24-8

MPT0L145

MPT0L145 is a selective inhibitor of PIK3C3 and FGFR, demonstrating a Kd value of 0.53 nM for PIK3C3. This compound effectively reduces phosphorylation of FGFR1 and FGFR3, along with their downstream signaling proteins, including FRS2, ERK, and Akt. MPT0L145 induces G0/G1 cell cycle arrest and downregulates cyclin E levels, leading to mitochondrial dysfunction, increased reactive oxygen species production, and DNA damage. As an autophagy inhibitor, MPT0L145 enhances the sensitivity of cancer cells to targeted therapies and chemotherapeutic agents, making it a valuable tool for research in cancer biology, particularly in bladder cancer and non-small cell lung cancer (NSCLC).