Catalog No.
Product Name
Application
Product Information
Citations
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FLT3-PROTAC Degrader
PROTAC FLT-3 degrader 4 is a CRBN-based degrader that selectively targets FLT3-ITD mutants by harnessing the ubiquitin-proteasome system for degradation. This compound demonstrates potent activity against FLT3-ITD mutant acute myeloid leukemia (AML) cells, offering a focused approach for research applications in cancer therapeutics. Its oral bioavailability positions it as a valuable tool for investigating FLT3-related signaling pathways and potential treatment strategies in AML. -
FLT3 Inhibitor
HI042 is a selective inhibitor of FMS-like Tyrosine Kinase 3 (FLT3), demonstrating potent activity with IC50 values of 0.62 μM in MOLM-13, 0.33 μM in MV4-11, and 0.89 μM in OCI-AML3 cell lines. This compound effectively reduces the viability of FLT3-internal tandem duplication (FLT3-ITD) mutation-positive cells, induces apoptosis, disrupts cell cycle progression, and diminishes clonogenic potential. HI042 serves as a valuable reagent in the research of acute myeloid leukemia (AML). -
IGF2BP2 Inhibitor
CWI1-2 is an inhibitor of IGF2BP2 that disrupts its interaction with m6A-modified target transcripts. This compound induces apoptosis and differentiation in responsive cells, showcasing potential anti-leukemic activity. CWI1-2 is valuable for research focused on the regulation of RNA metabolism and cancer biology, particularly in leukemia studies. -
TLR9 Agonist
Agatolimod is a Toll-like receptor 9 (TLR9) agonist and immunomodulator with an EC50 of 180 nM. It activates TLR9 and upregulates TLR6 expression, initiating downstream signaling through IRAK4, IRF5, and IRF7. Agatolimod enhances Th1-type immune responses and promotes the activation of various immune cells, leading to increased antigen presentation, antibody regulation, cytokine secretion, apoptosis, and enhanced cytotoxicity. This compound is relevant for research into COVID-19, breast cancer, lung adenocarcinoma, HPV-related tumors, melanoma, and salmonellosis. -
SERT/NET Inhibitor
Amitriptyline is a tricyclic antidepressant that primarily inhibits the serotonin transporter (SERT) and norepinephrine transporter (NET), enhancing synaptic levels of serotonin and norepinephrine. With a Ki value of 3.45 nM for SERT and 13.3 nM for NET, Amitriptyline demonstrates significant antidepressant activity. Additionally, it exhibits agonistic properties at α2A adrenergic and TrkA/TrkB receptors, contributing to its analgesic and neurotrophic effects. Furthermore, Amitriptyline interacts with various receptors, including muscarinic cholinergic and H1 receptors, which may lead to a variety of side effects, while its ability to block sodium channels and hERG potassium channels raises concerns regarding cardiotoxicity. -
ALKBH5 Inhibitor
DDO-2728 is a selective inhibitor of AlkB homologue 5 (ALKBH5), demonstrating an IC50 of 2.97 μM. This compound enhances the levels of N6 methyladenosine (m6A) modifications, leading to increased cell apoptosis and cell cycle arrest. DDO-2728 has shown efficacy in suppressing tumor growth in the MV4 11 xenograft model, highlighting its potential application in cancer research and therapeutic strategies targeting ALKBH5. -
IGF2BP1 Inhibitor
AVJ16 is an inhibitor of the insulin-like growth factor 2 mRNA binding protein IGF2BP1, exhibiting a Kd of 1.4 μM. This compound disrupts the interaction between IGF2BP1 and its target mRNA, thereby modulating gene expression and translation processes. AVJ16 is valuable for research applications focused on cancer cell migration and the underlying mechanisms of IGF2BP1 in various malignancies. -
ALK Inhibitor
Neladalkib is a potent oral selective inhibitor of anaplastic lymphoma kinase (ALK) with an IC50 of 2.8 nM. This compound induces apoptotic cell death and demonstrates anti-tumor activity, making it a valuable tool for cancer research. Neladalkib is particularly relevant in studies focused on ALK-driven malignancies and therapeutic resistance mechanisms. -
Ligand for E3 Ligase
Thalidomide 5-fluoride is a thalidomide-derived ligand for the E3 ubiquitin ligase Cereblon, enabling targeted protein degradation via the PROTAC approach. This compound can be conjugated with specific target protein ligands, such as IRAK4, to create PROTAC molecules for enhanced therapeutic applications. Notably, PROTAC IRAK4 degrader-1 demonstrated significant IRAK4 protein degradation in OCI-LY-10 cells at concentrations of 0.01, 0.1, and 1 μM, achieving degradation levels of <20%, >20-50%, and >50%, respectively. This underlines its potential utility in cellular studies of protein regulation and targeted therapeutics. -
IGF2BP3 Inhibitor
I3IN-002 is a small-molecule inhibitor of the RNA-binding protein IGF2BP3, exhibiting an IC50 of approximately 2 μM in SEM cells. By disrupting the interaction with m6A-modified mRNAs, I3IN-002 destabilizes the expression of key oncogenes, such as CDK6, MYC, and BCL2, leading to inhibition of leukemic cell proliferation, induction of cell cycle arrest, and promotion of apoptosis. This compound is a valuable tool for research focused on B-cell acute lymphoblastic leukemia. -
IRAK Inhibitor
KME-2780 is an orally active inhibitor targeting IRAK1 and IRAK4, exhibiting IC50 values of 19 nM and 0.5 nM, respectively. It plays a crucial role in the modulation of innate immune signaling pathways, making it a valuable tool for investigating dysregulation associated with hematologic malignancies and related disorders. Researchers can utilize KME-2780 to explore the therapeutic potential of IRAK inhibition in various immunological contexts. -
IGF2BP2 Inhibitor
CWI1-2 hydrochloride is an inhibitor of IGF2BP2, a protein that plays a crucial role in regulating m6A-modified target transcripts. By binding to IGF2BP2, CWI1-2 hydrochloride disrupts its interaction with these transcripts, thereby inducing apoptosis and promoting differentiation in cells. This compound demonstrates significant potential for therapeutic applications in leukemia research. -
IRAK4 PROTAC Degrader
PROTAC IRAK4 degrader-14 is an orally active degrader targeting IRAK4 with a DC50 of 2.4 nM. It functions by selectively degrading IRAK4, thereby inhibiting pro-inflammatory responses in various cell types, including T cells, monocytes, and keratinocytes. This compound has significant relevance in research focused on inflammatory diseases, particularly psoriasis. -
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. -
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. -
Src/Abl tyrosine kinase inhibitor
Bosutinib hydrate is an orally active Src/Abl tyrosine kinase inhibitor, demonstrating IC50 values of 1.2 nM and 1 nM for Src and Abl, respectively. This compound effectively disrupts signaling pathways involved in cell proliferation and survival, making it valuable for research in cancer biology, particularly in the study of chronic myeloid leukemia (CML) and other malignancies characterized by aberrant Src/Abl activity. Its potent inhibitory profile supports investigations into therapeutic interventions targeting these kinases. -
c-Kit Inhibitor
Imatinib-d8 is a deuterium-labeled derivative of Imatinib, a selective inhibitor targeting c-Kit and other tyrosine kinases, including BCR/ABL, v-Abl, and PDGFR. This compound exhibits potent anti-cancer activity by inhibiting kinase activity, making it a valuable tool for research in oncology and molecular biology. Its deuterium labeling allows for advanced tracking in pharmacokinetic studies and metabolic research. -
Src/Abl Inhibitor
Pro-Dasatinib is a potent Src/Abl kinase inhibitor that functions as an amino acid analog of Dasatinib. It exhibits significant antiproliferative activity against K652 leukemia cancer cells, with an IC50 of 0.21 nM. This compound serves as a valuable tool for research in cancer biology and therapeutic development, particularly in understanding and targeting pathways associated with leukemogenesis. -
Src-Abl Inhibitor
AP 24149 is a potent Src-Abl dual inhibitor that targets the Src and Abl kinases, exhibiting IC50 values of 9.1 nM and 3.6 nM, respectively. This compound demonstrates significant inhibitory activity against these kinases, making it a valuable tool for research in cancer biology and signal transduction. It is particularly useful in studies exploring the mechanisms of oncogenesis and therapeutic interventions in Src- and Abl-related 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. -
c-Src/Abl Inhibitor
BCR-ABL-IN-13 is a dual inhibitor of c-Src and Abl, exhibiting a Ki value of 0.55 μM against c-Src and 0.10 μM against wild-type Abl, with a Ki of 0.40 μM against the drug-resistant AblT315I mutant. This compound demonstrates competitive to mixed-type inhibition of wild-type Abl and non-competitive inhibition of the AblT315I mutant. BCR-ABL-IN-13 is suitable for research applications related to chronic myeloid leukemia, particularly in studies targeting resistant forms of the disease. -
FLT3 Inhibitor
MZH29 is a potent inhibitor targeting FLT3, demonstrating significant activity against both wild-type and various mutant forms, including FLT3-ITD, FLT3-D835H/Y/V, and FLT3-K663Q. Notably, MZH29 effectively inhibits the FLT3-ITD/F691L mutation, a known drug resistance variant associated with AC220. This compound is valuable for research in the field of oncology, particularly for studies related to acute myeloid leukemia (AML). -
c-KIT Inhibitor
Velzatinib is a selective inhibitor of c-KIT and targets multiple receptor tyrosine kinases including PDGFRB, PDGFRA, CSF1R, FLT3, and LCK. With IC50 values of 2.6 nM for PDGFRB and 44 nM for c-KIT, it demonstrates potent antitumor activity. Velzatinib has shown efficacy in xenograft mouse models, making it a valuable tool for cancer research and drug development targeting dysregulated growth signaling pathways. -
MER/FLT3 Inhibitor
UNC2025 hydrochloride is a potent ATP-competitive inhibitor targeting MER and FLT3, with IC50 values of 0.74 nM and 0.8 nM, respectively. It demonstrates over 45-fold selectivity for MERTK compared to Axl, exhibiting an IC50 of 122 nM and Ki of 13.3 nM. Its exceptional pharmacokinetic properties and ability to cross the blood-brain barrier make UNC2025 hydrochloride a valuable tool for investigating acute leukemia and related hematological conditions. -
CDK9/FLT3 Inhibitor
CDDD11-8 is a potent and selective inhibitor of cyclin-dependent kinase 9 (CDK9) and FLT3-ITD, exhibiting Ki values of 8 nM and 13 nM, respectively. This compound effectively reduces the proliferation of leukemia cell lines, particularly those associated with the FLT3-ITD mutation. CDDD11-8 serves as a valuable tool for research into targeted therapies for hematological malignancies, specifically in the study of cell cycle regulation and tyrosine kinase signaling pathways. -
FLT3 Inhibitor
FLT3-IN-17 is a potent FLT3 inhibitor, effectively targeting FLT3 mutants with an IC50 of less than 0.5 nM for the D835Y variant. Additionally, it exhibits inhibitory effects on focal adhesion kinase (FAK), with an IC50 value of 12 nM. This compound is valuable for research into cancer biology, particularly in the context of FLT3-driven malignancies and related pathways. -
IRAK1 Kinase Inhibitor
IRAK1/4/pan-FLT3 Kinase-IN-1 is a selective inhibitor targeting IRAK1, IRAK4, and FLT3 kinases, demonstrating IC50 values of 5 nM for IRAK1, 0.6 nM for IRAK4, and less than 0.5 nM for FLT3. This compound exhibits strong pharmacokinetic properties, indicating its potential for therapeutic application in acute myeloid leukemia research. Its efficacy in promoting survival suggests it may serve as a valuable tool for exploring novel treatment strategies in hematological malignancies. -
FLT3/AURKA Inhibitor
BPR1K871 is a potent dual inhibitor targeting FLT3 and AURKA, with IC50 values of 19 nM and 22 nM, respectively. This compound demonstrates significant anti-cancer activity and is suitable for preclinical development in oncology research. Its selective inhibition of these kinases makes it a valuable tool for studying FLT3 and AURKA-related signaling pathways in cancer. -
FLT3 Inhibitor
3-Hydroxy Midostaurin is an effective inhibitor of FMS-like tyrosine kinase-3 (FLT3), demonstrating autophosphorylation inhibition with IC50 values of approximately 132 nM in culture medium and 9.8 μM in plasma. This compound serves as a metabolite of PKC412 and exhibits greater cytotoxicity, albeit with reduced selectivity compared to its parent compound. It is particularly relevant in research focusing on hematological malignancies and FLT3-related signaling pathways. -
FLT3 Inhibitor
FLT3-IN-6 is a potent and selective FLT3-ITD inhibitor, demonstrating an IC50 of 1.336 nM. This compound effectively inhibits the mutated form of FLT3, making it a valuable tool in the study of hematological malignancies. Its specificity allows for precise exploration of FLT3-related pathways and potential therapeutic applications in cancer research. -
Dual FLT3/CHK1 Inhibitor
FLT3/CHK1-IN-1 is a dual inhibitor targeting both FLT3 and CHK1, demonstrating significant selectivity for c-KIT over other kinases. With an IC50 value of 58.4 μM, it shows reduced affinity for the hERG channel, minimizing potential cardiac side effects. FLT3/CHK1-IN-1 has exhibited efficacy in inhibiting tumor growth in mouse xenotransplantation models with MV-4-11 cells, making it a valuable tool for cancer research and therapeutic development. -
ITD-FLT3 Inhibitor
GTP-14564 is a selective inhibitor of the internal tandem duplication (ITD) variant of the FLT3 receptor tyrosine kinase. This compound effectively suppresses ligand-dependent proliferation of Ba/F3 leukemia cells, providing a valuable tool for the investigation of FLT3-related hematological malignancies. Its specificity may facilitate studies focused on the molecular mechanisms underlying FLT3-driven oncogenesis and therapeutic responses in leukemia. -
FLT3 Inhibitor
OTS447 is a potent inhibitor of FMS-like tyrosine kinase 3 (FLT3), exhibiting an IC50 value of 21 nM. This compound is primarily utilized in research focused on hematological malignancies, particularly acute myeloid leukemia (AML), where aberrant FLT3 signaling is implicated. OTS447 serves as a valuable tool in studies investigating FLT3-related pathways and potential therapeutic strategies targeting FLT3 mutations. -
FLT3 Inhibitor
Crenolanib benzenesulfonate is a potent and selective inhibitor of FLT3, including both wild-type and mutant isoforms, as well as PDGFRα and PDGFRβ. With dissociation constants (Kd) of 0.74 nM for FLT3 and 2.1 nM/3.2 nM for PDGFRα/β, it exhibits strong biological activity. This compound is primarily utilized in research applications focused on hematological malignancies and other cancers driven by aberrant receptor tyrosine kinase signaling pathways. -
PDGFRβ/B-Raf Inhibitor
KG5 is an orally active dual inhibitor targeting PDGFRβ and B-Raf through allosteric mechanisms. It also exhibits inhibitory effects on Flt3, KIT, and c-Raf. KG5 demonstrates significant anticancer and antiangiogenic activities, making it a valuable reagent for research in cancer therapy and angiogenesis studies.
