Catalog No.
Product Name
Application
Product Information
Citations
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ALK5/VEGFR2 Inhibitor
Tosposertib is a dual inhibitor targeting ALK5 and VEGFR2, with IC50 values of 1.2 nM and 4.9 nM, respectively. This compound effectively restores the functionality of cytotoxic T lymphocytes (CTLs) and natural killer cells that are suppressed by TGFβ, while concurrently inhibiting the activity and viability of regulatory T cells. Tosposertib is valuable for research applications related to melanoma and colon cancer. -
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 Degreder
AP-1 is a PROTAC designed to target anaplastic lymphoma kinase (ALK) for selective degradation. This compound comprises the target protein ligand CS-1243648, the E3 ligase ligand Pomalidomide, and a linker derived from 2-(Tert-Butoxy)-2-oxoacetic acid. AP-1 is valuable for research applications focused on studying ALK-related signaling pathways and the therapeutic potential of targeted protein degradation in cancer treatment. -
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. -
EML4-ALK PROTAC Degrader
PROTAC EML4-ALK Degrader-2 is an advanced degrader specifically targeting the EML4-ALK fusion protein. With an IC50 of 1.6 nM, it exhibits potent selective inhibitory activity against ALK while maintaining selectivity over IGF1R, INSR, FLT3, and FGFR2. This compound demonstrates significant anti-cancer effects in both in vitro and in vivo models and is particularly relevant for research applications involving non-small cell lung cancer (NSCLC), as well as liver and cervical cancers. -
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. -
Brigatinib-PROTAC Degrader
SIAIS117 is a potent Brigatinib-PROTAC degrader that targets the ALK protein, specifically effective against the ALK G1202R point mutation. By utilizing a VHL-1 conjugation, SIAIS117 exhibits significant capability to induce protein degradation, leading to inhibited growth of SR and H2228 cancer cell lines. This compound holds potential for applications in anti-proliferative research, particularly in small cell lung cancer contexts. -
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 Degrader
PROTAC ALK degrader-1 is a potent ALK degrader utilizing the proteolysis-targeting chimera (PROTAC) mechanism, exhibiting a DC50 of 26 nM in H3122 EML4-ALK cells. This compound enables selective degradation of ALK, thereby offering potential therapeutic benefits for ALK-driven cancers. Additionally, PROTAC ALK degrader-1 serves as a precursor for synthesizing PROTAC ALK degrader-2, which may possess enhanced bioavailability for further research applications. -
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 PROTAC Degrader
PROTAC ALK degrader-5 is a targeted degrader composed of a small molecule that selectively degrades anaplastic lymphoma kinase (ALK). It demonstrates potent inhibitory activity against EML4-ALK and NPM-ALK, with IC50 values of 27.4 nM and 116.5 nM, respectively. This compound exhibits significant anti-proliferative effects against ALK-driven cancer cell lines, including H3122 and Karpas 299, and effectively inhibits ALK and STAT3 phosphorylation. PROTAC ALK degrader-5 is a valuable tool for investigating ALK-driven malignancies, particularly in the context of human non-small cell lung cancer and anaplastic large cell lymphoma research. -
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 PROTAC Degrader
TD-004 is a highly effective ALK PROTAC degrader, demonstrating potent anti-ALK inhibitory activity with an IC50 of 0.11 µM. This compound selectively hampers the proliferation of ALK-positive cancer cell lines, SU-DHL-1 and H3122, with IC50 values of 0.058 µM and 0.28 µM, respectively. TD-004 induces the degradation of ALK fusion proteins, including NPM-ALK and EML4-ALK, through the recruitment of the VHL E3 ligase and the proteasome pathway. Its significant tumor growth inhibition and favorable safety profile in vivo make TD-004 a valuable tool for researching anaplastic large cell lymphoma and non-small cell lung cancer. -
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 ligand-Linker Conjugate
ALK ligand-Linker Conjugate 1 is designed to facilitate the synthesis of PROTAC ALK degrader-4, targeting the Anaplastic Lymphoma Kinase (ALK) pathway. This compound serves as a vital component in developing protein-targeting chimeras for therapeutic applications in cancer research. Its efficient linkage promotes effective degradation of ALK, making it a valuable tool for studies focused on modulating oncogenic signaling pathways. -
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 Ligand
ALK ligand-1 is a specific ligand for Anaplastic Lymphoma Kinase (ALK). It serves as a critical component in the synthesis of PROTAC ALK degrader-4, facilitating targeted protein degradation. This compound is valuable for research applications aimed at studying ALK-mediated pathways and developing novel therapeutic strategies in oncology. -
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-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.
