Catalog No.
Product Name
Application
Product Information
Citations
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FGFR Inhibitor
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. -
FGFR4 Inhibitor
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. -
FGFR1/2/4 Inhibitor
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. -
FGFR4 Inhibitor
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. -
FGFR2/3 Inhibitor
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. -
FGFR3 Inhibitor
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. -
FGFR Inhibitor
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. -
PIK3C3/FGFR Inhibitor
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). -
FGFR Modulator
FGFR-IN-7 is a potent fibroblast growth factor receptor modulator with oral bioavailability and effective blood-brain barrier penetration. It exhibits neuroprotective activity, making it a valuable tool for studying neurodegenerative diseases. Its ability to enhance brain exposure while reducing the risk of phospholipidosis emphasizes its potential in therapeutic applications related to CNS disorders. -
FGFR4 Inhibitor
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. -
FGFR1 Inhibitor
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. -
FGFR2/3 Inhibitor
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. -
FGFR1-3 Inhibitor
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. -
FGFR1 Inhibitor
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. -
FGFR1 Inhibitor
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. -
FGFR1 Inhibitor
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. -
FGFR Inhibitor
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. -
FGFR Inhibitor
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. -
Abl Kinase Inhibitor
AFG210 is a potent Abl kinase inhibitor with an IC50 of 330 nM, demonstrating significant inhibitory effects on additional kinases including B-Raf, C-Raf, FGFR-1, RET, and VEGF receptors. Its unique multi-target profile positions AFG210 as a valuable tool for investigating chronic myeloid leukemia and other disorders associated with aberrant Abl kinase activation. This compound facilitates research exploring targeted therapies and signaling pathways linked to these diseases. -
FGFR1/2/3/ CSF-1R Inhibitor
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. -
BCR-ABL PROTAC Degrader
Leu-PEG1-Dasa is an efficient BCR-ABL PROTAC degrader that operates through the N-terminal canonical pathway, demonstrating a DC50 of 0.48 nM. This compound utilizes a single amino acid as the E3 ligase ligand and exhibits significant anti-proliferative effects on K562 cells. Leu-PEG1-Dasa is applicable in the research of chronic myeloid leukemia (CML) and provides insights into targeted degradation mechanisms in cancer therapy. -
Bcr/Abl Kinase Inhibitor
PD166326 is a potent Bcr/Abl kinase inhibitor with an IC50 of 8 nM for Abl tyrosine kinase and 6 nM for Src tyrosine kinase. This compound effectively blocks Bcr/Abl kinase activity, leading to the inhibition of Bcr/Abl-dependent cell proliferation and cell cycle progression. In preclinical studies, PD166326 has demonstrated the ability to reduce peripheral blood granulocytosis, alleviate splenomegaly, and prolong survival in mouse models of chronic myeloid leukemia. It serves as a valuable tool for research focused on chronic myeloid leukemia and related signaling pathways. -
BCR-ABL1 Inhibitor
Asciminib hydrochloride is a potent and selective allosteric inhibitor targeting BCR-ABL1. This compound demonstrates significant biological activity by inhibiting Ba/F3 cells with an IC50 of 0.25 nM. Asciminib is primarily utilized in research applications focusing on chronic myeloid leukemia and other BCR-ABL1 driven malignancies, providing valuable insight into the mechanisms of resistance and therapeutic strategies. -
Bcr-Abl Inhibitor
Nilotinib-d6 is a deuterated form of Nilotinib, a selective inhibitor of the Bcr-Abl tyrosine kinase. This compound exhibits antineoplastic activity, making it valuable in the study of chronic myeloid leukemia and other malignancies characterized by Bcr-Abl expression. Nilotinib-d6 is particularly useful in pharmacokinetic studies and metabolic profiling due to its unique isotopic labeling. -
Bcr-Abl Inhibitor
AKE-72 is a potent Bcr-Abl inhibitor that selectively targets various BCR-ABL variants, including BCR-ABLWT, BCR-ABLT315, BCR-ABLE255K, BCR-ABLF3171, BCR-ABLH396P, and BCR-ABLQ252H, exhibiting IC50 values of less than 0.5 nM to 9 nM. This compound demonstrates significant anti-leukemic activity in the K-562 cell line, making it a valuable tool for research in hematological malignancies and targeted cancer therapies. AKE-72 holds potential for further studies investigating BCR-ABL-mediated signaling pathways and resistance mechanisms. -
ABL Inhibitor
BCR-ABL1-IN-1 is a selective ABL1 inhibitor with an IC50 of 8.7 nM. This compound is primarily utilized in research investigating diseases of the central nervous system (CNS). Its potent inhibitory action on ABL1 makes it an invaluable tool for studying ABL-related signaling pathways and their implications in various neurological disorders. -
Abl Inhibitor
PPY-A is an effective inhibitor of both wild-type and T315I mutant Abl kinases, exhibiting IC50 values of 9 nM and 20 nM, respectively. This compound also demonstrates inhibitory activity in Ba/F3 cells transformed with wild-type Abl and the T315I mutant, with IC50s of 390 nM and 180 nM, respectively. PPY-A is particularly relevant for research in chronic myeloid leukemia (CML), offering a valuable tool for investigating therapeutic strategies against this malignancy. -
ABL Kinase Inhibitor
BCR-ABL-IN-7 is a selective inhibitor of ABL kinases, including both wild-type and the T315I mutant forms. This compound demonstrates potent inhibitory activity against ABL kinases, making it a valuable tool in the study of chronic myeloid leukemia (CML). Researchers can utilize BCR-ABL-IN-7 to investigate mechanisms of resistance and explore therapeutic strategies in CML treatment. -
Bcr-Abl Inhibitor
BCR-ABL-IN-8 is a potent inhibitor of the BCR-ABL fusion protein. This compound features a trimethoxy group that enhances its activity against chronic myeloid leukemia (CML) cells. BCR-ABL-IN-8 can be utilized in research investigating the molecular mechanisms of CML and potential therapeutic strategies targeting BCR-ABL signaling pathways. -
Bcr-Abl Inhibitor
PROTAC BCR-ABL1 ligand 1, also known as compound GMB-475, is designed to selectively target the BCR-ABL1 oncoprotein. It functions as an allosteric inhibitor by recruiting the E3 ligase Von Hippel-Lindau, leading to the ubiquitination and subsequent degradation of BCR-ABL1. This mechanism of action supports research applications in cancer biology, particularly in studying resistance mechanisms in chronic myeloid leukemia (CML) and therapeutic strategies to overcome BCR-ABL1-mediated signaling. -
Bcr-Abl Inhibitor
BCR-ABL-IN-3 is a potent and irreversible inhibitor of the Bcr-Abl tyrosine kinase, exhibiting an IC50 of ≤100 nM against Ba/F3Bcr-AblT3151 cells. This compound demonstrates significant anti-cancer activity, making it valuable for research applications focused on chronic myeloid leukemia and other malignancies driven by Bcr-Abl mutations. Its use can aid in elucidating the molecular mechanisms of resistance and the development of targeted therapies. -
c-ABL Inhibitor
c-ABL-IN-1 is a selective inhibitor of c-Abl kinase, which plays a critical role in various cellular processes, including cell proliferation and survival. This compound demonstrates significant neuroprotective effects, making it a valuable tool in researching therapies for neurodegenerative diseases such as Parkinson's disease. Its ability to inhibit c-Abl specifically allows for targeted studies into the mechanisms underlying neurodegeneration and potential therapeutic interventions. -
ABL Inhibitor
DosatiLink-1 is a selective inhibitor of the Abelson murine leukemia (ABL) enzyme. It exhibits potent inhibitory activity against ABL, making it a valuable tool for studying ABL-related signaling pathways and its role in oncogenesis. This compound is useful in research focused on cancer biology and can aid in the development of targeted therapies for ABL-driven malignancies. -
c-Abl Inhibitor
WB-BC-15 is a selective c-Abl kinase inhibitor that effectively enhances radiation-induced germ-cell apoptosis. With an EC50 value of 10.5 μM, it demonstrates potential for use in cancer research, focusing on mechanisms of radio-sensitivity and apoptosis in germ cells. This compound may serve as a valuable tool for elucidating the role of c-Abl in therapeutic contexts involving radiation exposure. -
BCR-ABL Kinase Inhibitor
AP24163 is a selective BCR-ABL kinase inhibitor that effectively targets both wild-type BCR-ABL and the resistant variant BCR-ABL-T315I, with IC50 values of 7 nM and 511 nM, respectively. This compound serves as a valuable tool in the study of chronic myeloid leukemia (CML), enabling researchers to investigate the mechanisms of resistance and develop potential therapeutic approaches. -
c-Abl Inhibitor
c-ABL-IN-3 is a potent inhibitor of the c-Abl tyrosine kinase, a target implicated in multiple diseases, particularly cancer. This compound exhibits significant biological activity that may aid in the investigation of neurodegenerative disorders such as amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD) as well as various cancer types. Its utilization in research may facilitate a better understanding of c-Abl's role in disease progression and therapeutic interventions. -
Bcr-Abl Inhibitor
PD173956 is a pyridopyrimidine compound that selectively inhibits the Bcr-Abl kinase, particularly targeting the P-loop mutant form. This inhibitor demonstrates significant activity in blocking Bcr-Abl-mediated signaling pathways, making it valuable for research on chronic myeloid leukemia and other cancers driven by Bcr-Abl mutations. Its specificity and potency support investigations into therapeutic strategies aiming to overcome resistance encountered in kinase inhibitors. -
BCR-Abl PROTAC Degrader
GMB-805 is a potent BCR-Abl PROTAC degrader, demonstrating a DC50 of 30 nM in K562 cells. It effectively induces antiproliferative activity, making it a valuable tool for studying chronic myeloid leukemia. Additionally, GMB-805 exhibits significant anti-tumor efficacy in vivo, coupled with a favorable safety profile, highlighting its potential for therapeutic development. -
Bcr-Abl Kinase Inhibitor
BCR-ABL-IN-5 is a potent Bcr-Abl kinase inhibitor that demonstrates significant inhibitory activity against both wild-type Bcr-Abl and the T315I mutant, with IC50 values of 0.014 μM and 0.45 μM, respectively. This compound exhibits anti-proliferative effects on leukemic cells, making it a valuable tool in research related to chronic myeloid leukemia and related conditions. BCR-ABL-IN-5 is suitable for studies aimed at understanding the mechanisms of Bcr-Abl-mediated oncogenesis and developing targeted therapies. -
BCR-ABL Ligand
Asciminib-NH2 is a ligand targeting BCR-ABL, specifically involved in the modulation of oncogenic signaling pathways. This compound is crucial for the synthesis of proteolysis-targeting chimeras (PROTACs), including P19As, facilitating the targeted degradation of BCR-ABL fusion proteins. Its utility in research supports investigations into targeted cancer therapies and the mechanistic study of BCR-ABL related malignancies. -
mini-PROTAC BCR-ABL Degrader
Arg-PEG1-Dasa is a mini-PROTAC designed to selectively degrade BCR-ABL, a key oncogenic driver in chronic myeloid leukemia. It demonstrates potent degradation efficacy with an EC50 of 0.85 nM, and exhibits significant antiproliferative activity in K562 cells, with an IC50 of 0.36 nM. This reagent is valuable for research applications focused on targeted therapies for BCR-ABL-driven malignancies. -
BCR-ABL/SRC/p38 Inhibitor
CHMFL-ABL-053 is a potent, selective inhibitor targeting BCR-ABL, SRC, and p38 kinases, exhibiting IC50 values of 70 nM, 90 nM, and 62 nM, respectively. This compound demonstrates significant antiproliferative activity, making it a valuable tool in cancer research, particularly in studies focusing on chronic myeloid leukemia and related malignancies. Its oral bioavailability enhances its utility in in vivo research applications. -
ABL Inhibitor
DosatiLink-2 is an Abelson murine leukemia (ABL) enzyme inhibitor that functions by selectively inhibiting the kinase activity of the ABL protein. This compound demonstrates significant biological activity against ABL-driven malignancies, making it a valuable tool for research in cancer biology and therapeutic development. It is particularly useful in studies assessing the role of ABL in oncogenesis and resistance mechanisms in cancer treatment. -
BCR-ABL PROTAC Degrader
P19P is a BCR-ABL PROTAC degrader that demonstrates a DC50 value of approximately 20 nM for wild-type BCR-ABL protein. It effectively degrades various drug-resistant mutants, including T315I, E255K, H396R, and V468F, and exhibits significant anti-proliferative activity in BaF3-BCR-ABL (T315I) cells, with an IC50 of 13.1 nM against ABL (T315I). P19P is suitable for research applications related to chronic myeloid leukemia and acute lymphoblastic leukemia while showing no inhibition of vascular lumen formation in HUVEC cells. -
BCR-ABL PROTAC Degrader
SIAIS100 is a potent BCR-ABL PROTAC degrader, exhibiting a DC50 value of 2.7 nM. This compound facilitates the targeted degradation of the BCR-ABL fusion protein, making it an important tool in the study of chronic myeloid leukemia (CML). Its ability to induce proteolytic degradation offers valuable insights for therapeutic development and understanding disease mechanisms associated with CML. -
BCR-ABL PROTAC Degrader
SIAIS056 is a BCR-ABL PROTAC degrader that effectively targets and degrades BCR-ABL fusion proteins, displaying a potent DC50 value of 0.18 nM. It inhibits the BCR-ABL signaling pathway in a time-dependent manner, leading to reduced phosphorylation of BCR-ABL as well as downstream effectors like STAT5 and CRKL in K562 cells. Additionally, SIAIS056 demonstrates the ability to degrade various BCR-ABL resistance mutations and exhibits significant anti-proliferative effects, resulting in marked tumor regression in K562 xenograft models. This compound is valuable for research in leukemia. -
BCR-ABL PROTAC Degrader
P22D is a BCR-ABL PROTAC degrader designed for targeted protein degradation, exhibiting a DC50 value of approximately 10 nM for the wild-type BCR-ABL protein. This compound effectively inhibits the proliferation of K562 cells harboring the wild-type BCR-ABL, but does not exhibit activity against BaF3-BCR-ABL (T315I) cells. P22D is valuable for research on chronic myeloid leukemia and acute lymphocytic leukemia, offering insights into the mechanisms of resistance and targeted therapies. -
c-Abl Inhibitor
c-ABL-IN-2 is a selective inhibitor of c-Abl, a tyrosine kinase implicated in various pathologies, particularly cancer. This compound demonstrates significant potential for investigating neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS) and Parkinson's disease (PD). Additionally, c-ABL-IN-2 features an alkyne group, enabling it to function as a click chemistry reagent that can participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a valuable tool for chemical biology applications. -
Bcr-Abl Inhibitor
BCR-ABL-IN-6 is a selective Bcr-Abl kinase inhibitor targeting the Bcr-Abl fusion protein, with IC50 values of 4.6 nM for Bcr-AblWT and 227 nM for Bcr-AblT315I. It effectively inhibits Bcr-Abl kinase activity within cells, demonstrating an EC50 of 14.6 nM. As an imatinib derivative, BCR-ABL-IN-6 is applicable in research related to chronic myelogenous leukemia. Additionally, this compound features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, thus serving as a useful click chemistry reagent in various experimental contexts. -
c-Abl Inhibitor
c-ABL-IN-4 is a potent inhibitor of the c-Abl tyrosine kinase, a critical target in the treatment of various malignancies and neurodegenerative disorders. Inhibition of c-Abl has been associated with potential therapeutic effects in conditions such as amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD), as well as in cancer research. This compound facilitates the exploration of c-Abl’s role in disease pathology and therapeutic intervention strategies.
