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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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). -
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. -
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). -
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. -
EGFR inhibitor
(E)-AG 556 is a highly selective inhibitor of epidermal growth factor receptor (EGFR) that also exhibits anti-inflammatory activity by blocking lipopolysaccharide (LPS)-induced tumor necrosis factor-alpha (TNF-α) production. Its dual functionality makes it a valuable compound for investigating EGFR-driven signaling pathways as well as inflammation-related mechanisms. -
EGFR inhibitor
Pebezertinib (BLU-451) is an orally bioavailable epidermal growth factor receptor (EGFR) inhibitor with demonstrated central nervous system (CNS) penetration. It is specifically designed to target EGFR mutations, including exon 20 insertions, and is being investigated for the treatment of non-small cell lung cancer (NSCLC) harboring these alterations. Pebezertinib represents a promising therapeutic candidate for overcoming resistance in EGFR-driven NSCLC, particularly in cases with CNS involvement. -
EGFR Inhibitor
WB-308 is a small molecule EGFR inhibitor, designed to target the epidermal growth factor receptor and its associated signaling pathways. In vitro studies demonstrate that WB-308 effectively reduces the proliferation and clonogenicity of non-small cell lung cancer (NSCLC) cells, leading to G2/M phase arrest and apoptosis. Additionally, it demonstrates tumor growth inhibition in both lung orthotopic transplantation and patient-derived xenograft models. WB-308 was shown to impair the phosphorylation of EGFR, AKT, and ERK1/2 proteins, offering a promising alternative to existing EGFR-targeted therapies with potentially lower cytotoxicity. -
Dual COX-2/EGFR Inhibitor
Melafolone is a potent dual inhibitor of COX-2 and EGFR, displaying IC50 values of 13.2 μM for COX-2 and 17.4 μM for EGFR. This compound enhances the efficacy of anti-PD-1 therapy by promoting vascular normalization and downregulating PD-L1 through the PI3K/Akt signaling pathway in Lewis lung carcinoma (LLC) and CMT167 models. Melafolone is suitable for applications in lung cancer research. -
EGFR Mutant Inhibitor
EGFR-IN-176 is an orally active, ATP-competitive inhibitor specifically targeting mutant forms of the epidermal growth factor receptor (EGFR), notably the C797S-mediated triple mutant. This compound effectively suppresses AKT signaling pathways and induces apoptosis in Ba/F3 and PC-9 cell lines expressing the EGFR mutations EGFR19del/T790M/C797S and EGFRL858R/T790M/C797S. Selectivity is demonstrated by its lack of inhibition against wild-type EGFR-expressing A431 cells. Additionally, EGFR-IN-176 inhibits ALK enzymatic activity with an IC50 of less than 0.5 nM and serves as a valuable tool for research in non-small cell lung cancer (NSCLC). -
EGFR/HER2 Inhibitor
KU004 is a potent dual inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), exhibiting significant anticancer properties. This quinazoline derivative effectively inhibits the proliferation of human breast cancer SKBR3 cells through the induction of G1 phase cell cycle arrest. KU004 interferes with HER2 and EGFR activation, subsequently blocking downstream signaling pathways such as Akt and Erk, and promotes apoptosis primarily via the extrinsic pathway. Its mechanism makes it a valuable tool for cancer research, particularly in studies targeting breast cancer therapy. -
EGFR Inhibitor
EGFR kinase-IN-8 is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating strong inhibitory activity against both triple-mutated EGFR (L858R/T790M/C797S) and double-mutated EGFR (L858R/T790M), with IC50 values of 3.86 nM and 1.23 nM, respectively. This compound effectively suppresses EGFR phosphorylation, leading to inhibition of downstream signaling pathways, including AKT, STAT3, and MAPK. EGFR kinase-IN-8 has shown promising anticancer efficacy, particularly in the treatment of non-small cell lung cancer. -
EGFR/HER2 Inhibitor
Afatinib oxalate is a potent and irreversible dual specificity inhibitor of the ErbB family, specifically targeting EGFR and HER2. With IC50 values of 0.5 nM for EGFR wild-type, 0.4 nM for EGFR L858R, 10 nM for EGFR L858R/T790M, and 14 nM for HER2, it demonstrates strong inhibitory activity. This compound is primarily utilized in research on esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC), and gastric cancer, making it valuable for studies focused on these malignancies. -
EGFR Inhibitor
Lazertinib mesylate hydrate is a selective, irreversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It demonstrates high potency against both activating mutations and the T790M resistance mutation, effectively inhibiting the phosphorylation of EGFR, AKT, and ERK pathways. This compound induces apoptosis and suppresses tumor growth, particularly in non-small cell lung cancer models, making it valuable for research on brain metastases and targeted cancer therapies. -
EGFR Kinase Inhibitor
EGFR-IN-113 is an EGFR kinase inhibitor with an IC50 of 14.79 μM, effectively targeting the EGFR pathway. This compound induces apoptosis and inhibits cell proliferation through the downregulation of Akt and Erk1/2 signaling pathways. EGFR-IN-113 is suitable for research applications focused on EGFR-driven cancers, including lung, pancreatic, and breast carcinoma. -
PIM/PI3K/AKT/mTOR Inhibitor
IBL-302 is an orally available dual inhibitor targeting PIM and the PI3K/AKT/mTOR pathways. It exhibits significant antitumor activity against breast cancer and neuroblastoma, showing in vivo efficacy in nude mouse xenograft models by overcoming trastuzumab resistance. Additionally, IBL-302 enhances the cytotoxic effects of commonly used chemotherapeutic agents, including cisplatin, doxorubicin, and etoposide, making it a valuable compound for cancer research applications. -
EGFR Inhibitor
BI-4732 is a potent, orally active EGFR inhibitor that functions through reversible, ATP-competitive mechanisms. It selectively inhibits the kinase activity of mutant EGFR variants, including L858R, T790M, and C797S, with IC50 values of 1 nM, while sparing the wild-type EGFR. Furthermore, BI-4732 effectively reduces the phosphorylation of key signaling proteins such as AKT, ERK, and S6K. Its robust intracranial anti-tumor efficacy has been demonstrated in the YU-1097 xenograft model that harbors the EGFR_E19del/T790M/C797S mutation, making it a valuable tool for research in non-small cell lung cancer (NSCLC). -
EGFR Inhibitor
BAY 2476568 is a highly selective inhibitor of EGFR targeting exon 20 insertion variants. It demonstrates potent inhibition of the kinase activity of various EGFR exon 20 mutants, including insASV, insSVD, and insNPG, with IC50 values of 0.09 nM, 0.21 nM, and 0.11 nM, respectively. BAY 2476568 effectively reduces phosphorylation of EGFR (Y1068), ERK1/2, and Akt (S473) in Ba/F3 cells harboring these mutations. This compound is valuable for investigating non-small cell lung cancer (NSCLC) associated with EGFR exon 20 insertion mutations. -
EGFR Inhibitor
Lazertinib mesylate is a selective, irreversible inhibitor of the EGFR tyrosine kinase, designed for oral administration and capable of penetrating the central nervous system. It demonstrates high efficacy against both activating mutations and the T790M resistance mutation in EGFR. By inhibiting the phosphorylation of EGFR, AKT, and ERK, Lazertinib mesylate induces apoptosis and hampers tumor growth, as evidenced in mouse models of brain metastases. This compound is primarily utilized in research investigating non-small cell lung cancer. -
JAK2 Inhibitor
Itacnosertib is a selective inhibitor of JAK2, with an IC50 value of 8540 nM, and it also targets FLT3 and ACVR1 (ALK2) with an IC50 of 8 nM. This compound demonstrates significant anti-leukemic activity, making it valuable for research in hematological malignancies. Itacnosertib is utilized in studies investigating the mechanisms of JAK2-mediated signaling pathways and the development of targeted therapies for related disorders. -
EGFR Inhibitor
Delphinidin 3-glucoside chloride is an EGFR inhibitor known for its role in inducing apoptosis in B cell chronic lymphocytic leukaemia (B CLL). It demonstrates phytoestrogen activity by selectively binding to estrogen receptor beta (ERβ) with an IC50 of 9.7 μM and inhibits EGFR with an IC50 of 2.37 µM. Additionally, Delphinidin 3-glucoside chloride exerts antitumor effects through the pAKT/IRF1/HOTAIR pathway and provides protection against oxidative stress, as well as inhibiting platelet activation and endothelial dysfunction. This compound is useful in cancer research and studies related to hormonal regulation. -
JAK Inhibitor
JAK-IN-39 is a potent inhibitor of the Janus kinase (JAK) family, specifically targeting JAK1, JAK2, and JAK3 with IC50 values of 0.05, 1.18, and 0.03 nM, respectively. This compound effectively reduces the viability of TF-1 cells and inhibits the production of pro-inflammatory cytokines, including TNFα and IFNγ, in vitro. JAK-IN-39 is valuable for research into immune regulation and potential therapeutic applications in inflammatory diseases and hematological malignancies. -
STAT1/3 Inhibitor
STAT1/3-IN-1 is a potent inhibitor of STAT1 and STAT3, targeting the phosphorylation and nuclear translocation of these transcription factors. This compound demonstrates significant anti-inflammatory activity by reducing LPS-induced production of pro-inflammatory cytokines such as NO, IL-1β, IL-6, and TNF-α, as well as inflammatory mediators like iNOS and COX-2. STAT1/3-IN-1 exhibits low toxicity in murine models, making it a valuable tool for investigating neuroinflammation and its underlying mechanisms. -
ErbB-2/EGFR Inhibitor
Lapatinib ditosylate monohydrate is a selective inhibitor of the ErbB-2 and EGFR tyrosine kinase domains. It demonstrates potent biological activity with IC50 values of 10.2 nM against EGFR and 9.8 nM against ErbB-2. This compound is commonly utilized in cancer research to investigate mechanisms of tumor growth and resistance, particularly in breast cancer models. -
JAK/HDAC Inhibitor
JAK/HDAC-IN-3 is a dual inhibitor targeting Janus kinase (JAK) and histone deacetylases (HDAC). It exhibits potent inhibitory activity with IC50 values of 25.36 nM for JAK2, and 0.2 μM and 0.43 μM for HDAC and HDAC1, respectively. This compound is valuable for investigating the roles of JAK and HDAC pathways in cellular processes and disease models, particularly in cancer and inflammatory research. -
p-STAT3 Inhibitor
STAT3-IN-48 is a potent inhibitor of phosphorylated STAT3 (p-STAT3), functioning as a Sorafenib analogue. It effectively induces apoptosis in cancer cells through the inactivation of STAT3 via a SHP-1 dependent mechanism. Notably, STAT3-IN-48 does not inhibit general kinase activity, highlighting its specificity. This reagent is suitable for research applications focused on cancer biology and targeting STAT3 signaling pathways. -
JAK2/FLT3 Inhibitor
Flonoltinib TFA is a potent and orally bioavailable inhibitor that targets both JAK2 and FLT3, exhibiting IC50 values of 0.7 nM and 4 nM, respectively, alongside 26 nM and 39 nM for JAK1 and JAK3. This compound possesses significant anti-cancer activity, making it a valuable tool for research in oncology and therapeutic development against malignancies driven by these pathways. Its dual inhibition profile highlights its potential in addressing cancers associated with aberrant JAK2 and FLT3 signaling. -
Pim-1 Kinase Inhibitor
Pim-1 kinase inhibitor 2 specifically targets and inhibits Pim-1 kinase activity, a critical regulator of cell survival and proliferation. This compound has been demonstrated to induce apoptosis in various cell types, making it a valuable tool for cancer research. Its potent inhibitory effects on Pim-1 kinase provide insights into the molecular mechanisms of tumorigenesis and underscore its potential in therapeutic applications for cancer treatment. -
JAK2 Inhibitor
ZT55 is a potent and selective inhibitor of JAK2, exhibiting an IC50 value of 0.031 μM. This compound effectively inhibits the proliferation of JAK2V617F-expressing HEL cell lines, inducing apoptosis and cell cycle arrest. In vivo, ZT55 demonstrates significant efficacy in inhibiting the growth of HEL xenograft tumors in mouse models. It serves as a valuable tool for research in myeloproliferative neoplasms, including polycythemia vera and primary thrombocythemia.
