FGFR

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).

Cat. No.

A33573

CAS No.

2727083-99-8

CXF-007

CXF-007 is a selective inhibitor of fibroblast growth factor receptor 4 (FGFR4) with an IC50 value of 7 nM. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its specificity for FGFR4 positions it as a key reagent for studying FGFR4-mediated signaling pathways and exploring therapeutic options in FGFR4-driven malignancies.

Cat. No.

A33575

CAS No.

442534-83-0

FGFR1 inhibitor-14

FGFR1 inhibitor-14 is a selective inhibitor targeting the Fibroblast Growth Factor Receptor 1 (FGFR1). This compound demonstrates significant anti-proliferative activity in various cancer cell lines, making it a valuable tool in cancer research. It is particularly useful for studies focused on the role of FGFR1 signaling in tumorigenesis and therapeutic response.

Cat. No.

A33576

CAS No.

3025799-28-1

FGFR2/3-IN-2

FGFR2/3-IN-2 is a potent inhibitor of FGFR2 and FGFR3, demonstrating IC50 values of 3.7 nM and 31.2 nM, respectively, following a one-hour preincubation. This compound selectively inhibits FGFR2 and FGFR3 without affecting FGFR1/4 or other kinases, minimizing undesirable side effects such as diarrhea and elevated serum phosphate in vivo. FGFR2/3-IN-2 effectively induces tumor stasis or regression in the SNU-16 gastric cancer model, making it a valuable tool for research in cancer biology and targeted therapy.

Cat. No.

A33580

CAS No.

1035270-44-0

AZ8010

Synonyms: AZ12908010

AZ8010 is a selective inhibitor targeting fibroblast growth factor receptors 1 to 3 (FGFR1-3). It exhibits significant anti-proliferative activity, making it a valuable tool for cancer research. This compound can be utilized in studies exploring FGFR-related signaling pathways and their implications in tumorigenesis.

Cat. No.

A33581

CAS No.

459137-97-4

FGFR1 inhibitor-15

FGFR1 inhibitor-15 is a selective inhibitor of Fibroblast Growth Factor Receptor 1 (FGFR1), exhibiting an IC50 value of 27 μM. This compound is valuable for cancer research, facilitating the investigation of FGFR1 signaling pathways and their implications in tumor growth and development. Its use can contribute to the understanding of FGFR1-related oncogenic mechanisms and the potential for therapeutic targeting in malignancies.

Cat. No.

A33582

CAS No.

606958-57-0

FGFR1 inhibitor-16

FGFR1 Inhibitor-16 is a selective inhibitor of Fibroblast Growth Factor Receptor 1 (FGFR1). This compound demonstrates an inhibitory efficacy of 53.00% at a concentration of 50 μM and 24.95% at 10 μM. FGFR1 Inhibitor-16 is valuable for research applications focused on cancer, allowing for the exploration of FGFR1 signaling pathways and their roles in tumor biology.

Cat. No.

A33583

CAS No.

308298-51-3

FGFR1 inhibitor-17

FGFR1 inhibitor-17 is a potent inhibitor targeting fibroblast growth factor receptor 1 (FGFR1). This compound demonstrates significant anti-proliferative activity in various cancer models, making it a valuable tool for cancer research. Its ability to inhibit FGFR1 signaling pathways can aid in the investigation of tumor biology and the development of targeted therapies.

Cat. No.

A33585

CAS No.

848463-13-8

SSR128129E free acid

Synonyms: SSR free acid

SSR128129E free acid is an allosteric inhibitor of fibroblast growth factor receptors (FGFR), exhibiting an IC50 of 1.9 μM for FGFR1. This compound demonstrates significant biological activity in modulating FGFR signaling pathways, making it valuable for research into cancer and other diseases associated with FGFR dysregulation. Its oral availability further facilitates in vivo studies and therapeutic exploration.

Cat. No.

A33587

CAS No.

943189-02-4

FGFR-IN-12

FGFR-IN-12 is a selective inhibitor of the Fibroblast Growth Factor Receptor (FGFR). This pyrimidinyl aryl urea derivative exhibits potent inhibition of FGFR activity, making it a valuable tool for investigating pathways involving FGFR signaling. Its efficacy positions FGFR-IN-12 as a significant compound for research applications related to cancer biology and therapeutic development targeting FGFR-related diseases.

Cat. No.

A33590

CAS No.

2847066-15-1

Segigratinib hydrochloride

Synonyms: 3D185; HH185

Segigratinib hydrochloride is a selective inhibitor of FGFR1, FGFR2, FGFR3, and CSF-1R, exhibiting IC50 values of 0.5 nM, 1.3 nM, 3.6 nM, and 3.8 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its ability to target multiple receptors involved in tumor progression highlights its potential for therapeutic applications in oncology.

Cat. No.

A75530

CAS No.

34539-65-6

β,β-Dimethylacrylalkannin

Synonyms: Arnebin 1

β,β-Dimethylacrylalkannin is a potent inhibitor of Fibroblast Growth Factor Receptor 1 (FGFR1) with an IC50 value of 2.5 μM. By binding to the ATP pocket of FGFR1, it effectively disrupts downstream signaling pathways, leading to G2/M phase cell cycle arrest and subsequent necrosis and apoptosis in various cancer cell lines. This compound shows promising therapeutic potential in the treatment of malignancies such as hepatocellular carcinoma and colorectal cancer. Additionally, it serves as an adjuvant in the treatment of colistin-resistant Gram-negative bacterial infections, making it valuable for research in cancer therapy and antimicrobial resistance.

Cat. No.

B22012

CAS No.

2833703-74-3

FGFR3-IN-10

FGFR3-IN-10 is a selective inhibitor of fibroblast growth factor receptor 3 (FGFR3), demonstrating significantly enhanced specificity for FGFR3 compared to FGFR1. This compound is primarily utilized in cancer research and has applications in studying systemic sclerosis, fibrosis, and pulmonary fibrosis. Additionally, FGFR3-IN-10 is relevant for investigating genetic conditions such as achondroplasia, thanatophoric dysplasia, and severe achondroplasia with developmental delay, as well as Muenke syndrome and acanthosis nigricans (SADDAN).