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Catalog No.
Product Name
Application
Product Information
Citations
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FGFR Inhibitor
FGFR-IN-5 is a selective inhibitor of fibroblast growth factor receptor (FGFR), a critical tyrosine kinase receptor implicated in various cancer pathways. This compound demonstrates significant biological activity in inhibiting FGFR signaling, making it valuable for cancer research applications. Additionally, FGFR-IN-5 possesses an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), thus serving as a versatile click chemistry reagent for further molecular investigations. -
FGFR Inhibitor
FGFR-IN-11 is a potent covalent inhibitor of Fibroblast Growth Factor Receptors (FGFR), demonstrating IC50 values of 9.9 nM for FGFR1, 3.1 nM for FGFR2, 16 nM for FGFR3, and 1.8 nM for FGFR4. This compound effectively hinders the proliferation of various cancer cell lines at nanomolar concentrations and significantly reduces tumor growth in xenograft mouse models. FGFR-IN-11 serves as a valuable tool for research into targeted cancer therapies and the underlying mechanisms of FGFR-mediated tumorigenesis. -
FGFR4 Inhibitor
FGFR4-IN-12 is a selective inhibitor targeting Fibroblast Growth Factor Receptor 4 (FGFR4), demonstrating enhanced potency and specificity. This compound exhibits significant anti-proliferative effects against FGFR4-dependent hepatocellular carcinoma (HCC) cell lines, making it valuable for cancer research. Additionally, FGFR4-IN-12 features an alkyne functional group, enabling its use as a click chemistry reagent that can participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
FGFR Inhibitor
FGFR-IN-13 is an irreversible covalent inhibitor of fibroblast growth factor receptors (FGFR), specifically targeting FGFR1 (IC50 = 0.20 ± 0.02 nM) and FGFR4 (IC50 = 0.40 ± 0.03 nM). This compound modulates FGFR-mediated signaling pathways by downregulating total PARP and Bcl-2 protein levels while promoting the expression of Cleaved-PARP and Bax in a dose-dependent manner. FGFR-IN-13 exhibits significant antitumor activity, making it a valuable tool for cancer research and therapeutic applications involving FGFR signaling pathways. -
FGFR Inhibitor
FGFR-IN-22 is a potent FGFR inhibitor, demonstrating IC50 values of 0.631 nM for FGFR1, 1.26 nM for FGFR2, 0.851 nM for FGFR3, and 1 nM for FGFR4. This compound effectively inhibits cell proliferation linked to FGFR1 and FGFR3 signaling pathways, making it a valuable tool for research in cancer types such as chronic lymphocytic leukemia (CLL). FGFR-IN-22 is useful for studying the role of FGFRs in tumor biology and therapeutic development. -
FGFR4 Inhibitor
FGFR4-IN-6 is a covalent, reversible inhibitor of Fibroblast Growth Factor Receptor 4 (FGFR4), exhibiting an IC50 value of 5.4 nM. It demonstrates significant antitumor activity by inducing tumor regressions in a xenograft mouse model using the Hep3B2.1-7 hepatocellular carcinoma cell line, while maintaining a favorable toxicity profile. Additionally, FGFR4-IN-6 serves as a click chemistry reagent, featuring an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing compounds, making it a valuable tool for chemical biology applications. -
EGFR Inhibitor
EGFR-IN-47 is a potent orally active inhibitor of the EGFR L858R/T790M/C797S mutations, with an IC50 of 0.01 μM. This compound effectively induces cell cycle arrest and promotes apoptosis in cancer cells. EGFR-IN-47 holds significant potential for research applications related to non-small cell lung cancer (NSCLC). -
EGFR Inhibitor
EGFR-IN-78 is a reversible inhibitor of the EGFR variant C797S-TK, classified as a 2-aminopyrimidine derivative. This compound induces apoptosis and exhibits significant anti-proliferative activity by inhibiting EGFR phosphorylation. Additionally, EGFR-IN-78 effectively arrests the cell cycle at the G2/M phase, making it a valuable tool for research applications focused on targeted cancer therapies. -
EGFR-TK Inhibitor
EGFR-TK-IN-4 is a potent and selective inhibitor of the epidermal growth factor receptor tyrosine kinase (EGFR-TK). It has been demonstrated to induce apoptosis in cancer cells and exhibits significant antitumor activity. This compound is suitable for studying EGFR signaling pathways and developing targeted therapies in oncology research. -
EGFR Inhibitor
YS-363 is a potent and selective orally active inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 0.96 nM for wild-type and 0.67 nM for the L858R mutant form. This compound effectively induces G0/G1 cell cycle arrest and promotes apoptosis in target cells. YS-363 is valuable for research applications focused on cancer therapeutics and the molecular mechanisms of EGFR signaling. -
PDGFR Inhibitor
PDGFR-IN-1 is a potent inhibitor of the platelet-derived growth factor receptor (PDGFR), exhibiting IC50 values of 2.4 nM for PDGFRα and 0.9 nM for PDGFRβ. This compound demonstrates significant antitumor activity while maintaining low toxicity, making it a valuable tool for research applications in osteosarcoma studies. Its selectivity for PDGFR allows for detailed investigations into tumor growth mechanisms and therapeutic interventions. -
EGFRC797S-TK Inhibitor
Os30 is a potent fourth-generation EGFR inhibitor specifically targeting the EGFRC797S-TK mutation. With IC50 values of 18 nM and 113 nM for EGFRDel19/T790M/C797S TK and EGFRL858R/T790M/C797S TK, respectively, Os30 effectively inhibits EGFR phosphorylation, induces G1 phase cell cycle arrest, and triggers apoptosis in KC-0116 (BaF3-EGFRDel19/T790M/C797S) cells. This compound demonstrates significant antitumor activity in non-small cell lung cancer (NSCLC) harboring the EGFRC797S mutation, making it a valuable tool for cancer research and therapeutic exploration. -
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. -
FAK Inhibitor
FAK-IN-20 is a potent Focal Adhesion Kinase (FAK) inhibitor with an IC50 value of 0.27 nM. This compound demonstrates significant anticancer activity by inducing apoptosis and generating reactive oxygen species (ROS). Additionally, FAK-IN-20 is effective in arresting the cell cycle in the G2/M phase, making it a valuable tool for research in cancer biology and therapeutic strategies targeting FAK signaling pathways. -
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). -
VEGFR2/MET Inhibitor
Cabozantinib hydrochloride is a potent inhibitor of VEGFR2 and MET, exhibiting IC50 values of 0.035 nM and 1.3 nM, respectively. Additionally, it effectively inhibits other receptor tyrosine kinases including KIT, RET, AXL, TIE2, and FLT3 with IC50 values of 4.6 nM, 5.2 nM, 7 nM, 14.3 nM, and 11.3 nM. This compound demonstrates significant antiangiogenic properties by disrupting tumor vasculature and inducing apoptosis in both tumor and endothelial cells. It is widely utilized in cancer research to explore the mechanisms of tumor progression and treatment resistance. -
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. -
BTK Inhibitor
TM471-1 is a potent and covalent inhibitor of Bruton's tyrosine kinase (BTK), demonstrating an IC50 of 1.3 nM against BTKWT and exhibiting selectivity with IC50 values of >40,000 nM for BTKC481S, 7.9 nM for TEC, and 12.4 nM for TXK. This compound effectively inhibits cell proliferation both in vivo and in vitro, induces apoptosis, and causes arrest in the G0/G1 phase of the cell cycle. TM471-1 is valuable for research into the roles of BTK in various cancer types and related signaling pathways. -
ALK/ROS1 Inhibitor
Lorlatinib acetate is a selective and orally active inhibitor targeting ROS1 and ALK pathways. This compound exhibits potent anticancer activity with Kis of less than 0.025 nM for ROS1 and less than 0.07 nM for wild-type ALK, establishing it as a promising therapeutic candidate for ALK-driven cancers. Additionally, Lorlatinib acetate effectively inhibits ALK phosphorylation, demonstrated by IC50 values ranging from 15-43 nM for ALKL1196 and varying efficacy against multiple resistant mutations, making it a valuable tool for cancer research and drug discovery. -
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. -
VEGFR2/KDR Inhibitor
Vatalanib hydrochloride is a potent and selective inhibitor of VEGFR2 (vascular endothelial growth factor receptor 2), with an IC50 of 37 nM. It effectively penetrates the blood-brain barrier, making it suitable for studies involving central nervous system applications. Vatalanib hydrochloride is utilized in research focused on angiogenesis, tumor growth inhibition, and vascular biology, contributing valuable insights into therapeutic strategies for various cancers. -
FLT3 Inhibitor
Tuspetinib hydrate is a selective FLT3 inhibitor that demonstrates IC50 values of 1.1 nM, 1.8 nM, and 1.0 nM against FLT3 wild-type, FLT3 internal tandem duplication (ITD), and FLT3 D835Y kinases, respectively. As a reversible type I inhibitor, Tuspetinib hydrate effectively modulates key signaling pathways, including p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. This compound exhibits potent anti-leukemic activity by inhibiting cell proliferation and inducing apoptosis in leukemic cells, making it a valuable tool for research in leukemia and related hematological malignancies. -
FAK/FGFR2 Inhibitor
PHM16 is an ATP-competitive inhibitor targeting Focal Adhesion Kinase (FAK) and Fibroblast Growth Factor Receptor 2 (FGFR2), with IC50 values of 0.4 μM and 0.37 μM, respectively. This compound exhibits strong anti-angiogenic properties, making it a valuable tool for studies focused on inhibiting tumor angiogenesis and understanding related signaling pathways. Its dual inhibition profile positions PHM16 as an important reagent for cancer research and therapeutic development targeting angiogenesis-related mechanisms. -
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. -
ALK/EGFR Inhibitor
ALK/EGFR-IN-1 is a potent dual inhibitor targeting ALK and EGFR, effectively blocking their phosphorylation. This compound demonstrates high inhibitory activity against EGFR L858R T790M mutants in H1975 cells, with an IC50 of 4.3 nM, and EML4-ALK in BaF3 cells, with an IC50 of 3.6 nM. ALK/EGFR-IN-1 is particularly valuable for research in non-small cell lung cancer (NSCLC) and provides insights into the mechanisms of resistance in targeted therapies. -
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. -
VEGFR-2 Inhibitor
VEGFR-2-IN-15 is a selective inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2), a key regulator of angiogenesis. This compound effectively arrests cell growth in HepG2 cells at the Pre-G1 phase and induces apoptosis. It is a valuable tool for research applications focused on cancer biology and therapeutic strategies targeting angiogenesis. -
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). -
Syk Inhibitor
PRT-060318 dihydrochloride is a selective and potent inhibitor of the tyrosine kinase Syk, exhibiting an IC50 of 3 nM. This compound effectively suppresses B cell activation and migration in chronic lymphocytic leukemia (CLL) and induces apoptosis in these cells. Additionally, PRT-060318 dihydrochloride has demonstrated the ability to prevent Heparin-induced thrombocytopenia and thrombosis in transgenic mouse models, making it a valuable tool for research in CLL and thrombus formation. -
FLT3 Inhibitor
HI042 is a selective inhibitor of FMS-like Tyrosine Kinase 3 (FLT3), demonstrating potent activity with IC50 values of 0.62 μM in MOLM-13, 0.33 μM in MV4-11, and 0.89 μM in OCI-AML3 cell lines. This compound effectively reduces the viability of FLT3-internal tandem duplication (FLT3-ITD) mutation-positive cells, induces apoptosis, disrupts cell cycle progression, and diminishes clonogenic potential. HI042 serves as a valuable reagent in the research of acute myeloid leukemia (AML). -
ALKBH5 Inhibitor
DDO-2728 is a selective inhibitor of AlkB homologue 5 (ALKBH5), demonstrating an IC50 of 2.97 μM. This compound enhances the levels of N6 methyladenosine (m6A) modifications, leading to increased cell apoptosis and cell cycle arrest. DDO-2728 has shown efficacy in suppressing tumor growth in the MV4 11 xenograft model, highlighting its potential application in cancer research and therapeutic strategies targeting ALKBH5. -
ALK Inhibitor
Neladalkib is a potent oral selective inhibitor of anaplastic lymphoma kinase (ALK) with an IC50 of 2.8 nM. This compound induces apoptotic cell death and demonstrates anti-tumor activity, making it a valuable tool for cancer research. Neladalkib is particularly relevant in studies focused on ALK-driven malignancies and therapeutic resistance mechanisms. -
HIF-1α/Glutamate Inhibitor
Minocycline is a semi-synthetic tetracycline antibiotic that serves as a potent inhibitor of hypoxia-inducible factor (HIF)-1α, demonstrating significant anti-inflammatory and neuroprotective properties. In addition to its bacteriostatic effects through binding to the 30S subunit of bacterial ribosomes, Minocycline reduces glutamate neurotransmission, contributing to its antidepressant effects. This compound is employed in research applications focused on cancer, neurodegenerative diseases, and the modulation of inflammatory responses. -
HIF-1α inhibitor
PRLX-93936 dihydrochloride (Compound 16) is a small-molecule inhibitor of hypoxia-inducible factor 1α (HIF-1α) with demonstrated anticancer activity. It also suppresses signaling within the activated Ras pathway, thereby inhibiting tumor cell proliferation and survival. PRLX-93936 shows potential therapeutic relevance in the study of relapsed or refractory multiple myeloma and other Ras-driven malignancies, making it a useful compound for investigating hypoxia-related and oncogenic signaling mechanisms in cancer. -
Kinases PROTAC/Nek9 Inhibitor
DB0614 is a PROTAC molecule utilizing a cereblon ligand, designed as a selective and potent degrader of NEK9 and other kinases. It induces the degradation of multiple kinases, including ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1–3, MAP4K5, MAPK14, MAPK7–9, MAPKAPK2/3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1/3, SIK2/3, STK35, TNK2, and ULK1. DB0614 is suitable for research involving diseases or disorders driven by aberrant kinase activity. -
Menin-KMT2A inhibitor
Bleximenib (JNJ-75276617) is an orally active and highly selective menin–KMT2A (MLL) interaction inhibitor, with IC50 values of 0.1 nM in humans, 0.045 nM in mice, and ≤0.066 nM in dogs. It effectively inhibits the proliferation of tumor cells and induces apoptosis and differentiation, particularly in malignancies driven by KMT2A rearrangements. Bleximenib is a promising therapeutic candidate for the study and treatment of leukemia and other menin-dependent cancers. -
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. -
Menin-KMT2A inhibitor
Bleximenib (JNJ-75276617) oxalate is an orally active and highly selective inhibitor of the menin–KMT2A (MLL) interaction, with IC50 values of 0.1 nM in humans, 0.045 nM in mice, and ≤0.066 nM in dogs. It effectively inhibits tumor cell proliferation and induces apoptosis and differentiation, particularly in cancers driven by KMT2A rearrangements. Bleximenib oxalate is a promising candidate for research in leukemia and other menin–KMT2A-dependent malignancies. -
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). -
PDGFR Inhibitor
Methylnissolin (Astrapterocarpan), a natural compound isolated from *Astragalus membranaceus*, inhibits PDGF-BB-induced vascular smooth muscle cell proliferation with an IC50 of 10 μM. It exerts its effects by suppressing PDGF-BB-induced phosphorylation of ERK1/2, thereby blocking activation of the ERK1/2 MAP kinase signaling cascade. -
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. -
FLT3/CHK2 inhibitor
Lasmotinib (PHI-101) is a dual inhibitor of FLT3 and CHK2 with potent activity against FLT3 single activating mutations (ITD or TKD), as well as double (ITD/D835Y or ITD/F691L) and triple (ITD/D835Y/F691L) resistance mutations. It synergizes with Venetoclax or Azacytidine to enhance anti-leukemic effects and also demonstrates anticancer activity in ovarian and breast cancer models. -
FAK inhibitor
Ifebemtinib (BI-853520, IN-10018) is an orally active and potent inhibitor of focal adhesion kinase (FAK), with an IC50 of 1 nM against recombinant FAK. It exhibits antiproliferative activity in cancer cells and also inhibits FER and FES kinases, with IC50 values of 900 nM and 1040 nM, respectively. -
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).
