Catalog No.
Product Name
Application
Product Information
Citations
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Pan-HER Inhibitor
pan-HER-IN-2 is a reversible, orally active pan-HER inhibitor targeting multiple receptor tyrosine kinases, with IC50 values of 0.72 nM for EGFR, 2.0 nM for HER4, 8.2 nM for EGFRT790M/L858R, and 75.1 nM for HER2. This compound effectively induces apoptosis and exhibits significant antitumor activities. pan-HER-IN-2 is suitable for research applications focused on cancer therapy and the exploration of targeted treatments for HER family receptor-positive tumors. -
EGFR Inhibitor
Gefitinib dihydrochloride is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, exhibiting an IC50 of 33 nM. This compound effectively inhibits EGF-stimulated tumor cell proliferation (IC50 of 54 nM) and prevents EGFR autophosphorylation, thereby blocking downstream signaling pathways. Gefitinib dihydrochloride is valuable for cancer research, particularly in the study of lung and breast cancers, due to its ability to induce autophagy and promote apoptosis in tumor cells. -
EGFR Inhibitor
Zorifertinib hydrochloride is a potent orally active inhibitor of the epidermal growth factor receptor (EGFR), demonstrating IC50 values of 0.3 nM, 0.2 nM, and 0.2 nM against wild-type EGFR, EGFR L858R, and EGFR exon 19 deletion variants, respectively. This compound is capable of inducing apoptosis in cancer cells and exhibits significant antitumor activity. Zorifertinib hydrochloride is primarily utilized in research related to non-small cell lung cancer (NSCLC) and hepatocellular carcinoma (HCC). -
JAK2/FLT3 Inhibitor
Flonoltinib sulfate is a potent, orally active dual inhibitor targeting JAK2 and FLT3. It demonstrates significant biological activity with IC50 values of 0.7 nM for JAK2 and 4 nM for FLT3, along with activity against JAK1 and JAK3 at 26 nM and 39 nM, respectively. This compound is primarily utilized in cancer research, particularly in the study of hematological malignancies influenced by aberrant JAK2 and FLT3 signaling pathways. -
JAK1 Inhibitor
Ivarmacitinib sulfate is a selective inhibitor of the Janus kinase 1 (JAK1) pathway, exhibiting a significant preference over JAK2, JAK3, and Tyk2. This compound effectively inhibits JAK1-STAT3 phosphorylation, leading to the apoptosis of hepatic stellate cells. Ivarmacitinib sulfate demonstrates notable anti-proliferative and anti-inflammatory properties, making it a valuable tool for research on hepatic diseases and inflammation-related disorders. -
Aurora/JAK Inhibitor
AT9283 lactic acid is a multi-targeted kinase inhibitor primarily targeting Aurora A/B and JAK2/3. It demonstrates potent biological activity against various cancers, exhibiting IC50 values between 1 to 30 nM for its targets. AT9283 lactic acid effectively inhibits the growth and survival of multiple solid tumors in both in vitro and in vivo models, making it a valuable reagent for cancer research applications. -
c-kit/VEGFR/PDGFR Inhibitor
Famitinib malate is an orally active, multi-targeted kinase inhibitor primarily targeting c-kit, VEGFR-2, and PDGFRβ, with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively. This compound induces cell apoptosis and demonstrates significant anti-tumor activity in human gastric cancer cells and xenograft models. Famitinib malate is a valuable tool for research into cancer therapies and mechanisms of action. -
EGFR Inhibitor
SKLB188 is a potent and orally active inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 of 5 nM. This compound effectively suppresses both MEK/Erk and Akt/mTOR signaling pathways, leading to reduced proliferation of head and neck squamous cell carcinoma (HNSCC) and inducing caspase-dependent apoptosis. SKLB188 is a valuable reagent for research focused on EGFR-overexpressing solid tumors. -
EGFR Inhibitor
EGFR-IN-59 is an epidermal growth factor receptor (EGFR) inhibitor with an IC50 of 190 nM, demonstrating apoptosis-inducing properties. This compound exhibits significant cytotoxicity against non-small cell lung cancer cell lines (A549) with an IC50 of 8.62 µM, while maintaining a lower cytotoxic effect on normal lung fibroblasts (WI38) at 52.6 µM. EGFR-IN-59 is a valuable tool for investigating various cancers, including non-small cell lung cancer (NSCLC), head and neck cancer, breast cancer, and colorectal cancer. -
Pan-HER Inhibitor
pan-HER-IN-1 is an irreversible pan-HER inhibitor that targets multiple human epidermal growth factor receptors (HER) with IC50 values of 0.38 nM for EGFR, 1.6 nM for HER4, 2.2 nM for EGFRT790M/L858R, and 3.5 nM for HER2. This compound effectively induces apoptosis and exhibits significant antitumor activity, making it a valuable tool for cancer research and therapeutic applications aimed at HER-driven malignancies. -
STAT3 Inhibitor
STAT3-IN-38 is a selective inhibitor of the signal transducer and activator of transcription 3 (STAT3) protein, exhibiting a KD value of 45.33 µM. By binding to the SH2 domain of STAT3, it effectively inhibits phosphorylation at the pTyr705 site, leading to the downregulation of downstream genes such as Survivin and Mcl-1. This compound has demonstrated the ability to block cell-cycle progression and induce apoptosis in colorectal cancer cells, making it a valuable tool for cancer research and therapeutic development. -
AKR1B1/STAT3/SLC7A11-Regulator
AKR1B1/STAT3/SLC7A11-regulator-1 is a regulatory compound that targets the AKR1B1, STAT3, and SLC7A11 pathways to enhance ferroptosis activity. This mechanism effectively reverses doxorubicin resistance in MCF-7/ADR breast cancer cells. It serves as a valuable tool in breast cancer research, particularly for studies focused on overcoming chemotherapy resistance and exploring ferroptosis as a therapeutic strategy. -
JAK2/3 Inhibitor
JAK-2/3-IN-3 is a potent inhibitor of JAK2 and JAK3, demonstrating IC50 values of 13.00 nM and 14.86 nM, respectively. It effectively inhibits the autophosphorylation of JAK2 and promotes apoptosis in a dose- and time-dependent manner. This compound is valuable for research into lymphoid malignancies and leukemia, providing insights into the role of JAK signaling pathways in these diseases. -
GLUT1/EGFR Inhibitor
GLUT1/EGFR-IN-1 is a potent inhibitor of both the GLUT1 transporter and the EGFR tyrosine kinase. By targeting the ATP-binding site of EGFR and concurrently inhibiting GLUT1-mediated energy metabolism, GLUT1/EGFR-IN-1 effectively reduces ATP levels, mitochondrial membrane potential, and intracellular lactic acid, while also preventing EGFR nuclear translocation. This compound is applicable in research focusing on nasopharyngeal carcinoma (NPC) and triple-negative breast cancer (TNBC). -
IKK/STAT3 Dual Inhibitor
ACHP is a selective IκB kinase (IKK) and STAT3 dual inhibitor, demonstrating potent inhibitory activity with IC50 values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. It effectively disrupts the STAT3 signaling pathway, leading to cancer cell cycle arrest and apoptosis. Additionally, ACHP exhibits significant anti-inflammatory properties in preclinical models, such as the mouse ear edema model. This compound is a valuable tool for research in anti-inflammatory and anti-cancer studies, including applications in multiple myeloma and leukemia. -
HDAC3/p-STAT3 Inhibitor
1-Stearoyl-sn-glycero-3-phosphocholine is an inhibitor of histone deacetylase 3 (HDAC3) and the phosphorylation of signal transducer and activator of transcription 3 (p-STAT3). This compound has demonstrated the ability to induce apoptosis and exhibits significant anticancer activity in chronic myelogenous leukemia (CML) K562 cells. It serves as a valuable tool for researchers investigating the therapeutic potential of HDAC inhibitors in cancer treatment. -
JAK2 Inhibitor
Fedratinib hydrochloride hydrate is a selective, ATP-competitive inhibitor targeting the JAK2 kinase. With an IC50 of 3 nM for both JAK2 and the mutant JAK2V617F, it demonstrates significant potency. This compound exhibits 35-fold selectivity over JAK1 and 334-fold selectivity over JAK3. Fedratinib hydrochloride hydrate effectively induces apoptosis in cancer cells, making it a valuable tool for research in myeloproliferative disorders. -
STAT3/JAK Inhibitor
Brevilin A is a potent inhibitor of the STAT3/JAK signaling pathway, with an IC50 value of approximately 10.6 μM for STAT3. It exhibits anti-tumor properties and effectively inhibits the proliferation of cancer cells. Additionally, Brevilin A has been shown to induce both apoptosis and autophagy, making it a valuable tool for cancer research and therapeutic investigations. -
PKD/PIM2 Inhibitor
CRT0066101 is a potent and orally active inhibitor of Protein Kinase D (PKD) with IC50 values of 1 nM, 2.5 nM, and 2 nM for PKD1, PKD2, and PKD3, respectively. Additionally, it serves as an effective PIM2 inhibitor with an IC50 of approximately 135.7 nM. This compound exhibits notable anti-inflammatory activity demonstrated in LPS-induced lung injury models in mice, as well as anticancer effects, making it a valuable tool for research in cancer and inflammation-related studies. -
EGFR/HER2 inhibitor
Zongertinib (BI 1810631) is a potent and selective tyrosine kinase inhibitor targeting HER2 and EGFR, with IC50 values of 13 nM and 579 nM, respectively. It exhibits significant antitumor activity and is being investigated for the treatment of multiple solid tumors, particularly those driven by HER2 alterations. -
IL-23 receptor antagonist
Icotrokinra (JNJ-77242113) is an orally available and selective antagonist of the interleukin-23 (IL-23) receptor. It potently inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC₅₀ = 5.6 pM) and suppresses IL-23-induced interferon-γ (IFN-γ) production in natural killer (NK) cells (IC₅₀ = 18.4 pM). Icotrokinra also demonstrates anti-inflammatory activity in a rat TNBS-induced colitis model. It is a promising therapeutic candidate for the study and treatment of inflammatory conditions such as psoriasis, psoriatic arthritis, and inflammatory bowel disease (IBD). - 6-Demethoxytangeretin is a flavonoid compound isolated from *Citrus reticulata* with demonstrated anti-inflammatory and anti-allergic properties. It inhibits IL-6 production and the expression of related genes in human mast cells by modulating the ALK and MAPK signaling pathways. Additionally, 6-Demethoxytangeretin enhances CRE-mediated transcription in hippocampal neurons, indicating potential neuroregulatory effects.
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JAK2/FLT3 inhibitor
Flonoltinib is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM for JAK2, 4 nM for FLT3, 26 nM for JAK1, and 39 nM for JAK3. It exhibits strong anti-cancer activity and is a promising candidate for the treatment of hematologic malignancies and other JAK/FLT3-driven cancers. -
ALK/ROS1 inhibitor
Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor that effectively blocks tyrosine autophosphorylation of ALK, mutant ALK, and EGFR, with IC50 values ranging from 5.38 to 16.74 nM. Additionally, it inhibits the transport activity of MATE1, MATE2K, P-gp, and BCRP. Iruplinalkib is under investigation for the treatment of non-small cell lung cancer (NSCLC). - Gondoic acid (cis-11-Eicosenoic acid) is a monounsaturated long-chain fatty acid found in various plant oils and nuts. It exhibits anti-inflammatory activity by reducing reactive oxygen species (ROS) production and inhibiting the PKCθ/ERK/STAT3 signaling pathway. Gondoic acid is also utilized as a raw material in medical applications and as a moisturizing agent in cosmetic formulations.
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ADAM17 inhibitor
JG26 is a potent ADAM inhibitor with IC50 values of 12 nM for ADAM8, 1.9 nM for ADAM17, and 150 nM for ADAM10. It also inhibits MMP-12 with an IC50 of 9.4 nM. JG26 suppresses AngII-induced EGFR transactivation and ERK activation, upregulates ACE2 expression, inhibits CD23 shedding, and reduces SARS-CoV-2 infection. Additionally, JG26 demonstrates anti-metastatic effects in colorectal cancer and holds research potential in Hodgkin lymphoma and vascular diseases. -
Apoptosis activator
Sulforaphene, a natural compound isolated from radish seeds, exhibits an ED₅₀ of approximately 2 × 10⁻⁴ M against velvetleaf seedlings. It promotes apoptosis and inhibits migration in cancer cells by suppressing signaling pathways including EGFR, phosphorylated ERK1/2 (p-ERK1/2), and NF-κB. -
EGFR inhibitor
Avitinib (Abivertinib) maleate is a third-generation, irreversible, and orally active selective EGFR inhibitor with IC50 values of 0.18 nM for both EGFR^L858R and EGFR^T790M, and 7.68 nM for wild-type EGFR. In addition to its EGFR-targeting activity, Avitinib maleate also inhibits BTK phosphorylation and induces apoptosis in mantle cell lymphoma models, demonstrating broad-spectrum anticancer efficacy. -
EGFRC797S inhibitor
JND3229 is a reversible EGFR C797S inhibitor with IC50 values of 5.8 nM for EGFR^L858R/T790M/C797S, 6.8 nM for EGFR^WT, and 30.5 nM for EGFR^L858R/T790M. It exhibits potent antiproliferative activity and effectively suppresses tumor growth in vivo, making it a valuable tool for cancer research, particularly in the context of non-small cell lung carcinoma. -
EGFR inhibitor
Silevertinib (BDTX-1535, EGFR-IN-76) is an orally bioavailable, blood-brain barrier-permeable, and selective EGFR inhibitor with demonstrated antitumor activity. It has shown efficacy in preclinical models of non-small cell lung cancer (NSCLC), glioblastoma patient-derived tumors, and intracranial tumor models. -
EGFR inhibitor
Befotertinib (D-0316) mesylate is an orally active EGFR tyrosine kinase inhibitor that suppresses tumor cell proliferation. It is primarily investigated for its potential in treating EGFR T790M-positive non-small cell lung cancer (NSCLC). -
EGFR inhibitor
O-Desmethyl gefitinib is an active plasma metabolite of gefitinib, formed via CYP2D6-mediated metabolism. It retains EGFR inhibitory activity with an IC50 of 36 nM in subcellular assays. -
EGFR/PI3K Inhibitor
MTX-531 is an orally active small molecule that inhibits EGFR (IC50 = 14.7 nM) and multiple PI3K isoforms, with IC50 values of 6.4 nM (PI3Kα), 233 nM (PI3Kβ), 8.3 nM (PI3Kγ), and 1.1 nM (PI3Kδ), demonstrating potent antitumor activity. Additionally, MTX-531 functions as a weak PPARγ agonist (IC50 = 2.5 µM), which may mitigate PI3K inhibitor-induced hyperglycemia. -
EGFR inhibitor
Rezivertinib (BPI-7711) is an orally active, highly selective, and irreversible third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). It is designed to potently target both common activating EGFR mutations and the resistance-associated T790M mutation, which is a frequent cause of acquired resistance to earlier-generation TKIs. Rezivertinib also demonstrates excellent central nervous system (CNS) penetration, making it effective against brain metastases in EGFR-mutant non-small cell lung cancer (NSCLC). With its strong antitumor activity and favorable pharmacokinetic profile, Rezivertinib is a promising candidate for the treatment of EGFR-mutant NSCLC, particularly in patients with CNS involvement or T790M-driven resistance. -
pan-ErbB inhibitor
Dacomitinib (PF-00299804) hydrate is an orally active, irreversible pan-ErbB inhibitor targeting EGFR, HER2, and HER4. It potently inhibits ErbB family signaling pathways, suppressing tumor proliferation and survival. Dacomitinib hydrate is a valuable agent for research into cancers, particularly metastatic non-small cell lung cancer (NSCLC), where it demonstrates efficacy in targeting EGFR-driven oncogenesis. -
EGFR inhibitor
PP 3 (Compound 3) is an EGFR tyrosine kinase inhibitor with an IC50 of 2.7 μM. It targets the EGFR signaling pathway, which is critical for cell proliferation and survival in various cancers. PP 3 is a useful tool for research into EGFR-driven malignancies, such as non-small cell lung cancer and head and neck squamous cell carcinoma, enabling studies on tumor growth inhibition and potential therapeutic strategies. -
EGFR inhibitor
JBJ-09-063 hydrochloride is a highly potent, mutant-selective allosteric inhibitor of epidermal growth factor receptor (EGFR), specifically designed to target both TKI-sensitive and TKI-resistant EGFR mutations. It exhibits exceptionally low IC₅₀ values of: * 0.147 nM for EGFR L858R * 0.063 nM for EGFR L858R/T790M * 0.083 nM for EGFR L858R/T790M/C797S * 0.396 nM for EGFR^LT/L747S JBJ-09-063 hydrochloride effectively suppresses phosphorylation of EGFR and downstream signaling components, including Akt and ERK1/2, thereby inhibiting oncogenic signaling pathways. Its robust efficacy across a range of EGFR mutation profiles—including triple mutants that are resistant to third-generation TKIs—makes it a promising candidate for research and development in the treatment of EGFR-mutant non-small cell lung cancer (NSCLC). -
EGFR activator
Isoprocurcumenol is a guaiane-type sesquiterpene isolated from *Curcuma comosa* with notable bioactivity in epidermal growth factor receptor (EGFR) signaling. It activates EGFR and enhances downstream phosphorylation of ERK and AKT, key mediators of cell survival and proliferation pathways. As a result, isoprocurcumenol promotes keratinocyte proliferation, suggesting potential applications in skin regeneration, wound healing, and dermatological research. -
EGFR degrader
MS-39 is a highly potent and selective PROTAC degrader specifically engineered to target mutant forms of the epidermal growth factor receptor (EGFR). It is constructed by conjugating the EGFR inhibitor gefitinib to a von Hippel–Lindau (VHL) E3 ligase ligand via a tailored linker. MS-39 exhibits strong binding affinity and efficient degradation of mutant EGFR proteins, offering a promising strategy for overcoming resistance in EGFR-driven cancers. Its design enables targeted proteasomal degradation rather than mere kinase inhibition, providing a novel approach to cancer therapy. -
PROTAC JAK2 Degrader
SJ1008030 (compound 8) TFA is a selective JAK2-targeting PROTAC that promotes proteasomal degradation of Janus kinase 2 (JAK2). It exhibits potent antiproliferative activity in MHH–CALL-4 leukemia cells, with an IC₅₀ of 5.4 nM. By effectively eliminating JAK2 protein rather than merely inhibiting its activity, SJ1008030 TFA represents a promising therapeutic strategy for JAK2-driven hematologic malignancies, particularly in leukemia research. -
PROTAC EGFR degrader
MS9449 is a potent PROTAC-based degrader of the epidermal growth factor receptor (EGFR), exhibiting strong binding affinities with K\_d values of 17 nM for wild-type EGFR and 10 nM for the L858R mutant. It effectively induces degradation of mutant EGFR proteins via both the ubiquitin–proteasome system (UPS) and the autophagy–lysosome pathway, enabling dual-pathway clearance. MS9449 shows strong antiproliferative activity in non-small cell lung cancer (NSCLC) cells, making it a valuable compound for anticancer research, particularly in EGFR-driven tumors. -
Aurora Kinase A/JAK2 Inhibitor
AJI-214 is a dual-target inhibitor that simultaneously inhibits Aurora kinase A and Janus kinase 2 (JAK2). It directly blocks Aurora A activity, disrupting T cell mitotic progression and polarity, while also inhibiting JAK2-mediated STAT3 phosphorylation, thereby suppressing the differentiation of pro-inflammatory TH1 and TH17 cells. AJI-214 holds therapeutic potential for modulating immune responses and is being investigated for the prevention and treatment of graft-versus-host disease (GVHD). -
ErbB2 inhibitor
AG-825 is a selective, ATP-competitive inhibitor of ErbB2 (HER2) tyrosine kinase, with an IC₅₀ of 0.35 μM. It exhibits both anticancer and anti-inflammatory activities and has been shown to significantly accelerate apoptosis in human neutrophils. AG-825 also increases β₁-adrenergic receptor (β₁AR) density, suggesting potential cardiomodulatory effects. Due to its multifaceted biological activity, AG-825 is a valuable compound for research in oncology, inflammation, and cardiovascular disease. -
EGFR inhibitor
Limertinib (ASK120067) is a potent and orally active third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that selectively targets the EGFR^T790M resistance mutation with an IC₅₀ of 0.3 nM, while exhibiting reduced activity against wild-type EGFR (EGFR^WT, IC₅₀ = 6.0 nM). It is being investigated as a targeted therapy for non-small cell lung cancer (NSCLC) harboring EGFR-activating and resistance mutations. -
EGFR inhibitor
BLU-945 is a potent, highly selective, reversible, and orally bioavailable tyrosine kinase inhibitor (TKI) targeting mutant forms of the epidermal growth factor receptor (EGFR). It effectively inhibits EGFR variants harboring activating mutations such as L858R or exon 19 deletions, as well as resistance-associated mutations including T790M and C797S. BLU-945 is being developed as a next-generation therapeutic agent for the treatment of EGFR-mutant non-small cell lung cancer (NSCLC), particularly in cases resistant to earlier-generation EGFR inhibitors. -
EGFR inhibitor
CH7233163 is a noncovalent, ATP-competitive inhibitor that selectively targets the EGFR-Del19/T790M/C797S triple mutation, a known resistance mechanism to third-generation EGFR inhibitors such as Osimertinib. It effectively inhibits EGFR phosphorylation in Del19/T790M/C797S-mutant NIH3T3 cells and demonstrates significant antitumor activity in preclinical models. CH7233163 offers a promising therapeutic strategy for overcoming resistance in EGFR-mutant non-small cell lung cancer. -
ErbBs/BTK Inhibitor
Sunvozertinib (DZD9008) is a potent, orally active inhibitor of ErbB family kinases, including mutant forms of EGFR and HER2, as well as Bruton's tyrosine kinase (BTK). It demonstrates strong inhibitory activity against a range of clinically relevant EGFR mutations, with IC₅₀ values of 20.4 nM for EGFR exon 20 NPH insertion, 20.4 nM for EGFR exon 20 ASV insertion, 1.1 nM for EGFR L858R/T790M, and 7.5 nM for HER2 exon 20 YVMA mutation. It exhibits reduced activity against wild-type EGFR (IC₅₀ = 80.4 nM in A431 cells), supporting its selectivity for mutant forms. Sunvozertinib is being investigated as a targeted therapy for non-small cell lung cancers harboring EGFR or HER2 exon 20 alterations. -
EGFR inhibitor
Asandeutertinib (Osimertinib-d₃; AZD-9291-d₃) is a deuterated analog of Osimertinib, functioning as a tyrosine kinase inhibitor targeting the epidermal growth factor receptor (EGFR). It retains potent antineoplastic activity and is primarily used in research settings to study EGFR-driven cancers, particularly non-small cell lung cancer (NSCLC) with EGFR mutations, while offering potential advantages in pharmacokinetics due to deuterium substitution.
