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Catalog No.
Product Name
Application
Product Information
Citations
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ALK Inhibitor
CEP-28122 mesylate salt is a potent and selective inhibitor of Anaplastic Lymphoma Kinase (ALK), exhibiting an IC50 value of 1.9 nM. This diaminopyrimidine derivative demonstrates significant antitumor activity in preclinical models of ALK-positive human cancers. Its favorable pharmacodynamic and pharmacokinetic profiles support its use in research related to ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma. -
Trk/ROS1/ALK Inhibitor
Entrectinib-d8 is a deuterated derivative of Entrectinib, targeting TrkA/B/C, ROS1, and ALK receptors. This compound exhibits potent inhibitory effects with IC50 values of 1 nM for TrkA, 3 nM for TrkB, 5 nM for TrkC, and 12 nM for ROS1 and ALK. Entrectinib-d8 is effective in inducing apoptosis and cell cycle arrest in various cancer cell lines, demonstrating significant anti-tumor activity. Additionally, it has been shown to alleviate bleomycin-induced pulmonary fibrosis in murine models, making it a valuable tool for research in cancer and fibrosis therapies. -
ALK Inhibitor
Ficonalkib is a potent anaplastic lymphoma kinase (ALK) inhibitor that targets the tyrosine kinase receptor. It exhibits significant antineoplastic activity and is utilized in research to explore therapeutic strategies for ALK-driven malignancies. Its mechanism of action provides valuable insights into cancer biology and potential treatment pathways. -
Anaplastic lymphoma kinase (ALK) Inhibitor
ALK-IN-28 is a selective inhibitor of anaplastic lymphoma kinase (ALK), a critical target in various cancers, including non-small cell lung cancer and neuroblastoma. This compound effectively blocks ALK activity, demonstrating significant anti-proliferative effects in ALK-driven tumor models. ALK-IN-28 is suitable for research applications focused on elucidating ALK signaling pathways and exploring potential therapeutic strategies for ALK-positive malignancies. -
ALKBH5 Inhibitor
Ena15 is an inhibitor of the ALKBH5 enzyme, which plays a critical role in m6A RNA methylation. This compound enhances the demethylase activity of FTO, leading to increased levels of m6A-modified RNA and stabilization of FOXM1 mRNA. Ena15 demonstrates potent antitumor activity by suppressing the growth of glioblastoma multiforme, making it a valuable tool for research in cancer biology and therapeutic development. -
ALK Inhibitor
ALK Kinase Inhibitor-1 is a selective anaplastic lymphoma kinase (ALK) inhibitor, identified as compound I-202 from patent US20130261106A1. This compound exhibits potent inhibitory activity against ALK, a crucial target in various cancers, particularly those driven by ALK mutations such as non-small cell lung cancer. It is suitable for research applications aimed at studying ALK-related signaling pathways and evaluating potential therapeutic strategies in oncological contexts. -
EML4-ALK Inhibitor
EML4-ALK kinase inhibitor 1 is a potent inhibitor targeting the echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK), demonstrating an IC50 value of 1 nM. This compound effectively disrupts EML4-ALK signaling pathways, which are implicated in certain types of cancer, particularly non-small cell lung cancer. It serves as a valuable tool for research focused on understanding EML4-ALK-mediated oncogenic processes and exploring therapeutic strategies for EML4-ALK-positive malignancies. -
ALKBH5 Inhibitor
ALKBH5-IN-2 is a selective inhibitor of the ALKBH5 enzyme, demonstrating a potent inhibitory effect with an IC50 value of 0.79 µM. This compound has been shown to significantly reduce cell viability, making it a valuable tool for studying the role of ALKBH5 in various biological processes. Applications include investigations into cellular responses to RNA demethylation and exploring its implications in cancer research and epigenetic regulation. -
ALK Inhibitor
TL13-22 is a potent anaplastic lymphoma kinase (ALK) inhibitor with an IC50 of 0.54 nM. As a negative control for TL13-12, it serves as a valuable tool in research involving ALK pathways without inducing degradation of the ALK protein in cells. This compound can be utilized in studies focused on ALK-related cancers and signaling mechanisms. -
ALK Inhibitor
ALK-IN-5 is a highly potent and selective inhibitor of anaplastic lymphoma kinase (ALK), demonstrating an IC50 value of 2.9 nM. This compound effectively crosses the blood-brain barrier, making it suitable for research applications related to ALK-driven malignancies, particularly in neurological contexts. ALK-IN-5 serves as a valuable tool for investigating ALK signaling pathways and developing targeted therapies in cancer research. -
ALK Inhibitor
CJ-2360 is a highly selective and orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK), demonstrating IC50 values of 2.2 nM against wild-type ALK and various mutant forms, including F1197M, G1269A, L1196M, and S1206Y. This compound exhibits significant inhibitory activity against clinically relevant ALK mutants such as C1156Y and L1196M, as well as selectivity towards other kinases, including LTK, MERTK, CLK1, DAPK1, and DAPK2. CJ-2360 is suitable for studies focused on ALK-related cancers and the development of targeted therapies. -
ALK/EGFR Inhibitor
ALK/EGFR-IN-3 is a potent dual inhibitor targeting both ALK and EGFR. It demonstrates significant anti-proliferative effects on H1975, PC9, and Baf3-EML4-ALK cancer cell lines, with IC50 values of 0.1360, 0.0332, and 0.0339 μM, respectively. This compound is valuable for research in cancer biology, specifically for studying treatment resistance and therapeutic strategies in tumors characterized by ALK and EGFR alterations. -
ALK/ROS1 Dual Inhibitor
ALK/ROS1-IN-1 is a potent and selective dual inhibitor targeting ALK and ROS1, demonstrating IC50 values of 0.174 μM for ALK and 0.530 μM for ROS1. This compound is particularly effective against crizotinib-resistant variants, making it valuable for research applications focusing on cancer therapeutics and drug resistance mechanisms. Its ability to modulate these key oncogenic pathways makes it a significant tool for studying the therapeutic potential in various cancer models. -
ALK2 Inhibitor
ALK2-IN-5 is a pyrazolopyrimidine compound that selectively inhibits ALK2 activity, as well as FGFR activity. This compound demonstrates significant potential in research applications related to disorders influenced by dysregulated ALK2 and FGFR, including various cancer types. Its ability to modulate these key pathways makes it a valuable tool for investigating the molecular mechanisms underlying ALK2 and FGFR-related pathologies. -
ALK Inhibitor
ALK-IN-23 is a selective ALK inhibitor exhibiting IC50 values of 1.6 nM, 0.71 nM, and 1.3 nM against ALKWT, ALKL1196M, and ALKG1202R respectively. It effectively arrests the cell cycle in the G2 phase and promotes apoptosis in cancer cells. Additionally, ALK-IN-23 demonstrates the ability to inhibit cancer cell migration and colony formation in vitro, while revealing promising antitumor efficacy in H2228 xenograft models with low toxicity. This reagent is suitable for studies focused on ALK-related pathways and cancer therapeutics. -
ALK Inhibitor
Con B-1 is a potent and selective inhibitor of anaplastic lymphoma kinase (ALK), exhibiting low toxicity towards normal cells. This compound effectively modulates ALK activity, making it valuable for research into ALK-driven cancers. It is suitable for use in studies related to targeted therapies and evaluation of cancer cell proliferation and survival pathways. -
ALK Inhibitor
(E)-Belizatinib is a potent and selective anaplastic lymphoma kinase (ALK) inhibitor, exhibiting an enzymatic IC50 of 0.005 μM and a cellular IC50 of 0.048 μM. Demonstrating over 61-fold selectivity for ALK over JAK2, SRC, and IGF1R, (E)-Belizatinib possesses favorable pharmacokinetic properties in both rats and dogs. This compound is valuable for research focused on ALK-driven cancers, offering significant potential for therapeutic development in this area. -
ALK5 Inhibitor
ALK5-IN-79 is a selective ALK5 inhibitor that interferes with TGF-β1/SMAD signaling pathways, exhibiting significant anticancer activity. This compound reduces extracellular matrix production and collagen deposition, making it pertinent for studies focused on fibrosis and cancer progression. ALK5-IN-79 demonstrates favorable pharmacokinetic properties and good in vivo tolerance, supporting its potential as a therapeutic agent in various research applications. -
Anaplastic lymphoma kinase (ALK) Inhibitor
KRCA-0713 is a potent inhibitor of anaplastic lymphoma kinase (ALK), demonstrating robust anti-ALK activity in both enzyme and cell-based assays. This compound effectively suppresses ALK-driven tumor growth, as evidenced by studies conducted in H3122 xenograft models. KRCA-0713 serves as a valuable tool for researchers investigating ALK-related oncogenesis and therapeutic responses in cancer treatment. -
ALK Inhibitor
ALK5-IN-26 is a potent inhibitor of Activin receptor-like kinase 5 (ALK5), exhibiting an IC50 value of ≤10 nM. This compound is valuable for research applications investigating the role of ALK5 in cancer progression and related pathways. Its high specificity and efficacy make it a useful tool for elucidating the mechanistic underpinnings of tumor biology. -
ALK Inhibitor
WZH-15-125 is a potent anaplastic lymphoma kinase (ALK) inhibitor, showing significant activity against compound ALK mutations that contribute to drug resistance. With an IC50 of 101.7 nM, it effectively targets the G1202R/L1196M mutation, which demonstrates resistance to Lorlatinib. WZH-15-125 serves as a valuable ligand for PROTAC synthesis, specifically for the development of PROTAC WZH-17-002. This compound is particularly relevant for research in non-small cell lung cancer, offering new avenues for therapeutic exploration. -
ALK inhibitor
ALK-IN-13 is a selective inhibitor of anaplastic lymphoma kinase (ALK), targeting key pathways involved in oncogenesis. This compound exhibits potent anti-tumor activity, making it valuable for research focused on ALK-driven cancers, including non-small cell lung cancer. Its mechanism of action allows for detailed studies of ALK signaling and the development of targeted therapeutic strategies. -
ALK Inhibitor
F6524-1593 is an ALK inhibitor that demonstrates significant inhibitory activity against A549 and HepG-2 cell lines, with IC50 values of 161.1 μM and 91.03 μM, respectively. This compound is valuable for research involving ALK-related malignancies, including non-small cell lung cancer, lymphoma, and neuroblastoma. Its ability to selectively target ALK makes it a potential tool for understanding and developing treatments for these cancers. -
ALK Inhibitor
ALK-IN-21 is a potent inhibitor of the anaplastic lymphoma kinase (ALK), specifically targeting the ALKG1202R mutation. It demonstrates exceptional enzymatic inhibitory potency, with IC50 values of 4.59 nM for ALKWT, 2.07 nM for ALKL1196M, and 5.95 nM for ALKG1202R. This compound effectively inhibits the proliferation of ALK-positive Karpas299 and H2228 cell lines, exhibiting IC50 values of 0.07 μM. ALK-IN-21 is essential for research on anaplastic large cell lymphoma and related ALK-driven malignancies. -
ALK Inhibitor
ALK5-IN-29 is a selective inhibitor of activin receptor-like kinase 5 (ALK5), demonstrating potent inhibitory activity with an IC50 value of ≤10 nM. This compound has been shown to effectively inhibit tumor growth, making it a valuable tool for research in proliferative diseases, including cancer. Its specificity for ALK5 allows for targeted studies examining the role of this kinase in various biological processes and therapeutic interventions. -
ALK Inhibitor
Dirozalkib is a potent ALK inhibitor with an IC50 value of 0.9 nM. It demonstrates significant anti-proliferative activity in cancer cell lines, including NCI-H3122, Karpas-299, and NCI-H2228, with IC50 values of 130.4, 0.71, and 15.11 nM, respectively. Dirozalkib also possesses favorable pharmacokinetic properties, with a bioavailability of 30% to 50%, making it a valuable tool for research in cancer therapeutics. -
ALK Inhibitor
TL13-110 is a selective ALK inhibitor that demonstrates an IC50 of 0.34 nM. This compound serves as a negative control for TL13-112 while exhibiting minimal interaction with cellular ALK degradation. TL13-110 is suitable for research applications focused on the exploration of ALK-related pathways and therapeutic strategies in oncology. -
ALK2 Inhibitor
CDD-2789 is a highly selective small-molecule inhibitor of Activin receptor type 1 (ALK2, or ACVR1), which targets the SMAD1/5 signaling pathway. By effectively blocking ALK2/ALK1-mediated phosphorylation events triggered by BMP and activin A, CDD-2789 demonstrates a potent inhibitory effect with an IC50 of 0.54 µM in the NanoBRET cellular model. This compound is invaluable for research into ALK2-associated diseases, such as diffuse intrinsic pontine glioma (DIPG), ependymoma, endometrial cancer, melanoma, non-small cell lung cancer, colorectal cancer, and pancreatic cancer. -
ALK Inhibitor
KRCA-0377 is an orally active inhibitor of anaplastic lymphoma kinase (ALK) that demonstrates potent activity with an IC50 of 0.001 μM against the wild-type enzyme, and ≤0.01 μM for mutant forms. This compound exhibits significant cytotoxic effects against cancer cells and effectively inhibits tumor growth in xenograft mouse models. KRCA-0377 is suitable for research applications focusing on ALK-positive non-small-cell lung cancer. -
ALK/EGFR Inhibitor
ALK/EGFR-IN-2 is a potent dual inhibitor targeting anaplastic lymphoma kinase (ALK) and epidermal growth factor receptor (EGFR). This compound induces apoptosis and causes G0/G1 cell cycle arrest in cancer cells, contributing to its efficacy. It demonstrates significant inhibition of cell proliferation in H1975, PC9, and Baf3-EML4-ALK cancer cell lines, with IC50 values of 0.0034, 0.0065, and 0.0018 μM, respectively. ALK/EGFR-IN-2 is valuable for research focused on cancer therapeutics and pathway analysis. -
ALK Inhibitor
ALK-IN-12 is a potent and orally bioavailable inhibitor of Anaplastic Lymphoma Kinase (ALK), exhibiting an IC50 of 0.18 nM. In addition to its action on ALK, it also inhibits Insulin-like Growth Factor 1 Receptor (IGF1R) and Insulin Receptor (InsR), with IC50 values of 20.3 nM and 90.6 nM, respectively. The compound demonstrates significant antitumor activity, making it a valuable tool for cancer research focused on ALK-driven malignancies and cellular signaling pathways involving IGF1R and InsR. -
ALK Inhibitor
ALK5-IN-30 is a potent inhibitor targeting ALK5 and TGFβ-R1, demonstrating IC50 values of less than 10 nM for both proteins. This compound is invaluable for research applications involving modulation of the TGF-β signaling pathway, which plays a critical role in cellular processes such as proliferation, differentiation, and immune response. Its high affinity and selectivity make it an essential tool for studies focused on cancer, fibrosis, and other diseases influenced by ALK signaling. -
ALK5 Inhibitor
J-1048 is a selective inhibitor of activin receptor-like kinase 5 (ALK5). It effectively inhibits TGF-β/Smad signaling, thereby reducing TAA-induced liver fibrosis in murine models. This compound is valuable for studying the roles of TGF-β signaling in fibrotic diseases and for evaluating therapeutic strategies targeting liver fibrosis. -
ALKBH5 Inhibitor
DDO-02267 is a selective covalent inhibitor of ALKBH5, demonstrating an IC50 value of 0.49 μM. This compound enhances N6-methyladenosine (m6A) levels and modulates the ALKBH5-AXL signaling pathway. DDO-02267 serves as an important tool for elucidating the biological functions of mRNA demethylase in various research contexts. -
ALK Inhibitor
ALK-IN-9 is a highly potent inhibitor of anaplastic lymphoma kinase (ALK), demonstrating exceptional efficacy in inhibiting cell proliferation with IC50 values of less than 0.2 nM across multiple cell line models, including Ba/F3-EML4-ALK and KG-1 (OP2-FGFR1). This compound is particularly valuable in research applications focused on targeting ALK-driven cancers and exploring the role of ALK in various signaling pathways. Its robust biological activity makes it a critical tool for studying therapeutic resistance and drug development strategies in oncology. -
ALK5 Inhibitor
PF-03671148 is a selective inhibitor of ALK5, a receptor kinase involved in TGFβ signaling. This compound effectively attenuates TGFβ-induced fibrotic gene expression in fibroblasts, making it a promising candidate for research on fibrosis and related conditions. PF-03671148 may hold significant potential for therapeutic applications aimed at preventing dermal scarring and modulating fibrotic responses in various tissues. -
ALK2 Inhibitor
LDN-193688 is a selective inhibitor of ALK2, exhibiting IC₅₀ values of 104, 18, 235, 1530, and 1080 nM against ALK1, ALK2, ALK3, ALK4, and ALK5, respectively. This compound effectively inhibits bone morphogenetic protein 4 (BMP4)-induced phosphorylation of SMAD1/5/8, with an IC₅₀ of 2.6 μM. LDN-193688 is utilized in research focused on the BMP signaling pathway and its role in various biological processes, including development and disease. -
ALK/ROS1 Inhibitor
ALK/ROS1-IN-4 is a selective dual inhibitor targeting the anaplastic lymphoma kinase (ALK) and ROS1 kinases. This compound exhibits potent inhibitory activity against both kinases, making it a valuable tool for studying signaling pathways involved in certain cancers. ALK/ROS1-IN-4 is primarily used in research applications focused on cancer biology and therapeutic development for ALK- and ROS1-positive malignancies. -
ALK Inhibitor
CEP-28122 mesylate hydrochloride is a selective, orally active inhibitor of the anaplastic lymphoma kinase (ALK) with a reported IC50 of 1.9 nM. Exhibiting significant antitumor activity, it is effective in experimental models of ALK-positive malignancies, including anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma. Its favorable pharmacodynamic and pharmacokinetic properties make it a valuable tool for research into ALK-driven cancers. -
ALK inhibitor
Alectinib analog is a selective inhibitor of Anaplastic Lymphoma Kinase (ALK), specifically designed to overcome resistance via gating mutations. This compound shows low micromolar IC50 values, indicating potent antiproliferative and cytotoxic effects against cancer cells. Its efficacy is linked to enhanced stability and the release of active components. Additionally, Alectinib analog has been demonstrated to inhibit vascular septal dimensions in an in vivo zebrafish model, highlighting its potential for therapeutic applications in cancer research. -
c-FMS(CSF-IR)/c-Kitdual Inhibitor
Vimseltinib is a selective dual inhibitor of c-FMS (CSF-IR) and c-Kit, demonstrating IC50 values of less than 0.01 μM and 0.1-1 μM, respectively. This compound exhibits robust biological activity, making it a valuable tool for investigating signaling pathways involved in hematopoiesis and various pathologies such as cancer and inflammatory diseases. The oral bioavailability of Vimseltinib enhances its potential for in vivo studies and therapeutic applications. -
c-kit Inhibitor
Bezuclastinib is a highly selective inhibitor of the c-kit tyrosine kinase, demonstrating potent activity against the KIT D816V mutation. This compound is valuable for researching nonadvanced systemic mastocytosis (NonAdvSM) and provides insight into the underlying mechanisms of this condition. Its oral bioavailability makes it a convenient option for in vivo studies targeting c-kit dysregulation. -
CSF1R Inhibitor
Pimicotinib is a selective and orally active inhibitor of the Colony Stimulating Factor 1 Receptor (CSF1R), with an IC50 value of 19.48 nM as determined by the inhibition of ADP production. This compound demonstrates significant anti-tumor activity, making it a valuable tool for research applications aimed at understanding tumor microenvironment interactions and immune modulation. Researchers can utilize Pimicotinib to explore CSF1R-mediated signaling in cancer biology and potential therapeutic strategies. -
Tyrosine Kinase Inhibitor
Elenestinib is a selective orally active tyrosine kinase inhibitor, demonstrating a potent inhibitory effect on the KIT D816V mutant with an IC50 value of 6 nM. Its mechanism of action is primarily focused on inhibiting aberrant signaling pathways associated with systemic mastocytosis. Due to its limited ability to cross the blood-brain barrier, Elenestinib is particularly applicable in the investigation of hematologic disorders related to mast cell proliferation and activity. -
c-Kit Inhibitor
c-Kit-IN-5 is a potent c-Kit inhibitor, demonstrating IC50 values of 22 nM in kinase assays and 16 nM in cellular assays. This compound exhibits over 200-fold selectivity for c-Kit compared to other kinases, such as KDR, p38, Lck, and Src. Due to its favorable pharmacokinetic properties, c-Kit-IN-5 is well-suited for research applications exploring c-Kit-related signaling pathways and their implications in various diseases, including cancer. -
c-Kit/PDGFR Inhibitor
Labuxtinib is a potent dual inhibitor of c-Kit and PDGFR, effectively blocking cell proliferation driven by c-Kit or PDGFR signaling pathways. This compound is suitable for research applications targeting mast cell-associated diseases, respiratory conditions, inflammatory disorders, fibrosis, and metabolic diseases. Its dual mechanism of action makes Labuxtinib a valuable tool for investigating the molecular underpinnings of these diseases and potential therapeutic strategies. -
VEGFR/PDGFα/c-Kit Inhibitor
Telatinib mesylate is a potent, orally active inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit, exhibiting IC50 values of 6 nM, 4 nM, 15 nM, and 1 nM respectively. This compound effectively impedes angiogenesis and tumor cell proliferation, making it a valuable tool in cancer research. Its selective targeting of key signaling pathways has potential applications in studying tumor microenvironments and in developing therapeutic strategies for various malignancies. -
Tyrosine Kinase Inhibitor
Elenestinib phosphate is an orally active tyrosine kinase inhibitor that selectively targets the KIT D816V mutation, exhibiting an IC50 of 0.2 nM. This compound's targeted inhibition is particularly relevant for studying systemic mastocytosis, as it provides insights into the role of mutated KIT in this condition. Notably, elenestinib phosphate has limited capacity to penetrate the blood-brain barrier, making it suitable for investigating its effects in peripheral tissues. -
c-KIT/PDGFR/RET Inhibitor
KBP-7018 is a selective tyrosine kinase inhibitor targeting c-KIT, PDGFR, and RET. It demonstrates potent inhibition with IC50 values of 10 nM for c-KIT, 7.6 nM for PDGFR, and 25 nM for RET. This compound is valuable for investigating the molecular mechanisms and potential treatments related to idiopathic pulmonary fibrosis. -
c-Kit Inhibitor
c-Kit-IN-7 is a potent c-Kit inhibitor that demonstrates an IC50 of ≤10 nM. It effectively inhibits cell proliferation in GIST430 and BaF3 mutant cell lines, with IC50 values of ≤100 nM. This compound is crucial for research focused on cancers driven by c-KIT kinase mutations, providing valuable insights into therapeutic strategies targeting this pathway.
