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Catalog No.
Product Name
Application
Product Information
Citations
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ALK Inhibitor
ALK/PI3K/AKT-IN-1 is a selective ALK inhibitor that demonstrates significant anti-proliferative effects on A549, H1975, and PC9 cancer cell lines with IC50 values of 0.44, 0.83, and 1.51 μM, respectively. This compound induces cell cycle arrest at the G1 phase by enhancing p21 and p27 expression while inhibiting CDK2 and phosphorylated Rb activity. Additionally, ALK/PI3K/AKT-IN-1 disrupts the ALK/PI3K/AKT signaling pathway, leading to mitochondrial membrane depolarization and apoptosis in A549 cells. It also effectively inhibits spheroid formation and growth in A549 cells, making it a valuable tool for cancer research. -
FLT3 Inhibitor
FLT3-IN-32 hydrochloride is a potent and orally bioavailable inhibitor of FLT3, demonstrating IC50 values of 0.29 nM, 0.77 nM, and 2.07 nM against the FLT3-ITD, FLT3-D835Y, and FLT3-N676K mutations, respectively. This compound effectively reduces FLT3 phosphorylation and inhibits downstream signaling pathways such as STAT5, MAPK, and AKT, ultimately leading to apoptosis in FLT3-mutated Ba/F3 cells. Additionally, FLT3-IN-32 hydrochloride exhibits significant anti-tumor efficacy in the MV4-11 xenograft model, making it a valuable tool for investigations into acute myeloid leukemia (AML). -
IGF-1R/IR Inhibitor
GTx-134 is a dual inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR), exhibiting IC50 values of 97 nM and 187 nM, respectively. This compound effectively inhibits IGF-1R autophosphorylation and downstream Akt signaling, thereby interfering with the proliferation and survival of tumor cells. GTx-134 demonstrates broad-spectrum activity against multiple myeloma cell lines, inducing apoptosis in sensitive cells, and significantly reduces tumor growth in mouse models of myeloma. Its potential for synergistic effects with existing therapies makes GTx-134 a valuable reagent for high-risk myeloma research. -
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. -
ALK Inhibitor
ALK-IN-31 is an orally active inhibitor of anaplastic lymphoma kinase (ALK), with an IC50 of 1135 nM. This compound demonstrates significant antiproliferative activity against H2228 lung cancer cells, showing an IC50 of 1.35 μM. ALK-IN-31 induces apoptosis and halts cell cycle progression in the G0/G1 phase by modulating mitochondrial function. Furthermore, it attenuates tumor growth by downregulating p-AKT and p-mTOR within the PI3K-AKT-mTOR signaling pathway, making it a valuable tool for research in non-small cell lung cancer (NSCLC). -
VEGFR-2 Inhibitor
VEGFR-2-IN-77 is a selective inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), displaying an IC50 value of 139 nM. This compound effectively disrupts the PI3K/AKT/mTOR signaling pathway, leading to cytotoxic effects specifically in leukemia and prostate cancer cells. VEGFR-2-IN-77 induces cell cycle arrest and apoptosis while inhibiting cell migration and invasion. It serves as a valuable tool for investigating therapeutic strategies in leukemia and prostate cancer research. -
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. -
ACK1 Inhibitor
Ack1 Inhibitor 1 is a selective and orally active inhibitor of ACK1 kinase, exhibiting an IC50 value of 2.1 nM. This compound effectively inhibits the phosphorylation of ACK1, subsequently blocking the activation of downstream AKT signaling. Ack1 Inhibitor 1 demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic exploration. -
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. -
FLT3 Inhibitor
FLT3-IN-34 is a selective FLT3 inhibitor, exhibiting an IC50 value of 1.4 nM. It effectively blocks FLT3 phosphorylation and disrupts downstream signaling pathways involving AKT and ERK1/2. FLT3-IN-34 induces a concentration-dependent G0/G1 phase arrest and promotes mild apoptosis in FLT3-ITD-positive MV4-11 cells, demonstrating potent anti-proliferative effects with IC50 values of 14.95 nM and 18.5 nM against MV4-11 and MOLM-13 cell lines, respectively. This compound is suitable for investigating FLT3-positive acute myeloid leukemia (AML) and understanding FLT3-related signaling mechanisms. -
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). -
Src/Akt Inhibitor
Chrysotoxine is a dual inhibitor of the Src and Akt signaling pathways. It effectively suppresses cancer stem cell phenotypes by down-regulating the Src/Akt pathway, leading to reduced cell viability and increased apoptosis in H460 and H23 cancer cell lines, while sparing non-tumor cell lines. Due to its rapid excretion and low bioavailability in animal studies, Chrysotoxine serves as a valuable tool in cancer research, particularly for investigating therapies targeting cancer stem cells. -
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. -
FLT3-ITD Inhibitor
Clifutinib is a selective inhibitor of the FLT3-ITD mutation, exhibiting an IC50 of 15.1 nM. This compound demonstrates potent antiproliferative effects against FLT3-ITD acute myeloid leukemia (AML) cell lines, with IC50 values of 1.5 nM and 1.4 nM for MV-4-11 and MOLM-13, respectively. Clifutinib disrupts FLT3-ITD kinase activity, subsequently inhibiting downstream RAS/MAPK, PI3K/AKT, and JAK/STAT5 signaling pathways, leading to apoptosis in FLT3-ITD-positive AML cells. Additionally, it shows significant antitumor efficacy in mouse models bearing MV-4-11 or MOLM-13 xenografts, making it a valuable tool for investigating relapsed/refractory FLT3-ITD-positive AML. -
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. -
IGF Signaling Pathway Inhibitor
Chromeceptin (94G6) is an inhibitor of the Insulin-like Growth Factor (IGF) signaling pathway. It effectively suppresses IGF2 expression at both mRNA and protein levels in hepatocytes and hepatocellular carcinoma (HCC) cells. Additionally, Chromeceptin reduces the phosphorylation of key signaling proteins, AKT and mTOR, thereby impacting cellular growth and metabolism. This compound is valuable for research into cancer biology and therapeutic strategies targeting IGF signaling. -
IRAK4 Inhibitor
IRAK4-IN-33 is a selective and potent inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4), exhibiting an IC50 of 0.36 nM. This compound effectively disrupts the pro-inflammatory signaling pathway associated with IRAK4, leading to decreased release of inflammatory cytokines such as TNFα and IFNα. IRAK4-IN-33 demonstrates minimal inhibition of the hERG channel, with an IC50 greater than 30 μM, making it a valuable tool for studying inflammation and immunological disorders, including rheumatoid arthritis. -
RAF/DDR Inhibitor
PHI-501 is a dual inhibitor targeting RAF and DDR pathways. It demonstrates potent anti-proliferative effects in melanoma cell lines, effectively inhibiting colony formation in drug-resistant cells. PHI-501 disrupts ERK and AKT phosphorylation and downregulates key gene sets associated with TNFA-NFKB, IL6-JAK-STAT3, and KRAS signaling pathways, as well as pathways involved in epithelial-mesenchymal transition. In vivo studies show significant anti-tumor efficacy in the SK-MEL3DR xenograft model, making PHI-501 valuable for research on drug resistance in melanoma. -
IRAK4 Inhibitor
GLPG4471 is a selective inhibitor of IRAK4, demonstrating an IC50 of 1.7 nM. It exhibits potent inhibition of cytokine secretion, including TNFα and IFNα, in both cellular and whole blood assays. Notably, GLPG4471 shows significant therapeutic activity in a mouse model of collagen-induced arthritis, making it a valuable tool for researching inflammatory conditions such as arthritis. -
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. -
VEGFR Inhibitor
Gamabufotalin is a selective inhibitor of the Vascular Endothelial Growth Factor Receptor (VEGFR). This compound, derived from the traditional Chinese medicine Chansu, exhibits potent anti-cancer properties by significantly suppressing cancer cell proliferation and modulating inflammatory responses. Its ability to inhibit angiogenesis is primarily attributed to the blockade of VEGFR-2 signaling pathways, making it a valuable tool for research in cancer therapies and vascular biology. -
PDGFR Inhibitor
Sennoside B is a potent inhibitor of platelet-derived growth factor receptor (PDGFR). It effectively suppresses cell proliferation and reduces the phosphorylation of PDGFR-β, STAT-5, AKT, and ERK in response to PDGF-BB stimulation. Additionally, Sennoside B exhibits gastroprotective properties and is suitable for research applications focused on gastritis and related gastrointestinal disorders. -
VEGFR Inhibitor
Chloropyramine hydrochloride is an H1 histamine receptor antagonist that also serves as an inhibitor of vascular endothelial growth factor receptor 3 (VEGFR-3) and focal adhesion kinase (FAK). This compound exhibits key biological activities, contributing to research in angiogenesis and related pathways. It is valuable for studies aimed at understanding the role of VEGFR signaling in various physiological and pathological processes. -
FLT3 Inhibitor
Dovitinib lactate hydrate is a multi-targeted tyrosine kinase inhibitor primarily targeting FLT3. It exhibits potent inhibitory activity with IC50 values of 1 nM for FLT3, making it a valuable tool for research in hematological malignancies. In addition to FLT3, it also inhibits c-Kit, FGFR1/3, VEGFR1/2/3, and PDGFRα/β, facilitating studies focused on various signaling pathways and cancer therapeutics. -
FLT3 Inhibitor
CHMFL-FLT3-122 is a selective FLT3 kinase inhibitor with an IC50 of 40 nM. It demonstrates significant selectivity for FLT3 over BTK and c-KIT, exhibiting IC50 values of 421 nM and 559 nM, respectively. This compound effectively induces apoptosis through cell cycle arrest in the G0/G1 phase, making it a valuable tool for research in hematological malignancies and targeted cancer therapies. -
FLT3 Inhibitor
Tandutinib hydrochloride is a potent and selective inhibitor of FLT3, with an IC50 of 0.22 μM. This compound also exhibits inhibitory activity against c-Kit and PDGFR, with IC50 values of 0.17 μM and 0.20 μM, respectively. Its primary applications include research in acute myelogenous leukemia (AML). Additionally, Tandutinib hydrochloride demonstrates the ability to cross the blood-brain barrier, making it a valuable tool in studying central nervous system involvement in malignancies. -
c-MET Kinase Inhibitor
Capmatinib hydrochloride is a selective c-MET kinase inhibitor that competitively targets ATP (IC50 = 0.13 nM). It effectively inhibits the phosphorylation of c-MET and its downstream signaling pathways, including ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib hydrochloride demonstrates potent antitumor activity by inhibiting c-MET-dependent tumor cell proliferation and migration, as well as inducing apoptosis. This compound is primarily metabolized by CYP3A4 and aldehyde oxidase, making it relevant for studies in cancer research and therapeutic development. -
c-MET Inhibitor
ABN401 is a selective ATP-competitive inhibitor of c-MET, exhibiting an IC50 of 10 nM. This compound demonstrates cytotoxic effects on MET-addicted cancer cells, with IC50 values ranging from 2 to 43 nM. ABN401 has shown oral bioavailability in preclinical models, with 42.1% to 56.2% in rats and 27.4% to 37.7% in dogs, and possesses significant antitumor activity, making it a valuable tool for cancer research and therapeutic development. -
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. -
PDGFRα/β/Bcr-Abl Inhibitor
GZD856 formic is a selective inhibitor of PDGFRα/β, displaying IC50 values of 68.6 nM and 136.6 nM, respectively, along with potent inhibition of Bcr-Abl, including the T315I mutant with IC50s of 19.9 nM and 15.4 nM. This compound exhibits notable antitumor activity, making it a valuable tool for cancer research. Additionally, GZD856 formic serves as a click chemistry reagent due to its alkyne group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating bioconjugation studies and compound labeling. -
EGFR Inhibitor
T-1-PMPA is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating significant apoptotic effects. This compound effectively targets both wild-type EGFR (EGFRWT) and the EGFR 790M mutation, exhibiting IC50 values of 86 nM and 561.73 nM, respectively. T-1-PMPA is suitable for research applications focused on cancer biology and therapeutic efficacy in EGFR-related pathways. -
EGFR Inhibitor
Khellin is a furochromone that acts as an inhibitor of the epidermal growth factor receptor (EGFR) with an IC50 of 0.15 µM. It demonstrates significant anti-proliferative activity in vitro, making it a valuable compound for cancer research. Additionally, Khellin exhibits antispasmodic properties and coronary vasodilator effects, further broadening its potential applications in biological studies. -
EGFR Tyrosine Kinase Inhibitor
Olmutinib hydrochloride is an orally active and irreversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. By covalently binding to a cysteine residue in the kinase domain, it effectively disrupts signaling pathways associated with non-small cell lung cancer (NSCLC). This compound is utilized in research to study the mechanisms of EGFR-related oncogenesis as well as potential therapeutic strategies for NSCLC treatment. -
Mutant-Selective EGFR Inhibitor
Osimertinib mesylate is a mutant-selective inhibitor of the epidermal growth factor receptor (EGFR), acting through a covalent and irreversible mechanism. It demonstrates potent biological activity with an apparent IC50 of 12 nM against the L858R mutation and 1 nM against the L858R/T790M mutation. Osimertinib mesylate is primarily utilized in research focused on overcoming T790M-mediated resistance to existing EGFR-targeted therapies in lung cancer. -
EGFR Inhibitor
Almonertinib mesylate is an orally available, irreversible third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. It exhibits potent inhibitory activity against T790M, T790M/L858R, and T790M/Del19 variants, with IC50 values of 0.37 nM, 0.29 nM, and 0.21 nM, respectively, while demonstrating reduced efficacy against wild-type EGFR (3.39 nM). This compound is primarily utilized in the study of non-small cell lung cancer for its potential to overcome resistance in patients with specific EGFR mutations. -
EGFR Inhibitor
STX-721 is an orally active, irreversible covalent inhibitor of the EGFR exon 20 insertion (ex20ins) mutants, specifically targeting their unique dynamic protein states. This compound effectively inhibits the kinase activity of ex20ins mutants, such as NPG, ASV, and SVD, leading to a reduction in phosphorylation of EGFR and downstream ERK signaling. In cellular assays, STX-721 suppresses the proliferation of ex20ins-mutant Ba/F3 cells and human non-small cell lung cancer (NSCLC) cell lines. Additionally, it demonstrates tumor regression in patient-derived xenograft models, making it a valuable tool for studying NSCLC with EGFR or HER2 ex20ins mutations. -
EGFR Inhibitor
Befotertinib is an orally active EGFR tyrosine kinase inhibitor targeting the epidermal growth factor receptor. It exhibits significant antitumor activity by inhibiting the proliferation of tumor cells, making it relevant for research applications in EGFR T790M-positive non-small cell lung cancer (NSCLC). This compound facilitates the investigation of therapeutic strategies for NSCLC and enhances understanding of resistance mechanisms associated with EGFR mutations. -
EGFR/SKP2 Inhibitor
NSC689857 is a potent inhibitor of the epidermal growth factor receptor (EGFR) and the SCF(SKP2) complex, exhibiting an IC50 of 36 μM for Skp2-Cks1. This compound effectively inhibits the ubiquitylation of p27 with an IC50 of 30 μM. NSC689857 demonstrates variable activity across different cancer types, showing particularly enhanced efficacy against leukemia cell lines, making it a valuable tool for cancer research focusing on EGFR-related pathways and cell cycle regulation. -
EGFR Inhibitor
EGFR-IN-61 is a selective inhibitor of the epidermal growth factor receptor (EGFR) kinase, exhibiting IC50 values of 42 nM for the L858R/T790M variant, 137 nM for L858R/T790M/C797S, and 743 nM for the wild type. It demonstrates significant antiproliferative effects against A549 and H1975 cell lines, with IC50 values of 2.14 μM and 1.82 μM, respectively. This compound is useful for investigating EGFR-related signaling pathways and therapeutic interventions in cancer research. -
Mutant EGFR/HER2 Inhibitor
EGFR/HER2-IN-14 is a highly selective inhibitor of mutant forms of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) that exhibit resistance to conventional therapeutic agents. This compound demonstrates significant anti-cancer activity, making it a valuable tool for research focused on tumorigenesis and resistance mechanisms in various cancer types. Its use can facilitate the investigation of targeted therapies in cancer research, particularly in patient-derived models expressing these mutant receptors. -
EGFR/VEGFR2 Inhibitor
EGFR/VEGFR2-IN-4 is an irreversible inhibitor targeting the epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor 2 (VEGFR-2). It exhibits potent inhibitory activity with IC50 values of 18.7 nM for EGFR and 102.3 nM for VEGFR-2 in the presence of 1 μM ATP. This compound is valuable for research applications focused on cancer therapeutics and angiogenesis, providing insights into signaling pathways and potential treatment strategies. -
EGFR Inhibitor
EGFR-IN-132 is a potent inhibitor of the epidermal growth factor receptor (EGFR), effectively targeting both wild-type and various mutant forms, including L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S, with IC50 values of 1.6 nM and lower. This compound demonstrates favorable pharmacokinetic properties and high oral bioavailability, making it suitable for in vivo studies. EGFR-IN-132 holds significant potential for research applications involving cancer therapy, particularly in models of EGFR-driven malignancies. -
EGFR/HER2 Inhibitor
EGFR/HER2-IN-8 is a potent inhibitor of the EGFR and HER2 kinases, as well as dihydrofolate reductase (DHFR), displaying IC50 values of 0.45 μM, 0.244 μM, and 5.669 μM, respectively. This compound demonstrates significant anticancer activity against multiple cancer cell lines while maintaining a favorable safety profile and selectivity. EGFR/HER2-IN-8 is a valuable tool for investigating therapeutics targeting cancer pathways and can contribute to further understanding of cancer biology. -
Raf/EGFR Inhibitor
Lifirafenib maleate is a potent inhibitor of Raf kinase and EGFR, exhibiting IC50 values of 23 nM and 29 nM for recombinant BRafV600E and EGFR, respectively. This compound effectively disrupts critical signaling pathways involved in cancer cell proliferation and survival. Lifirafenib maleate is relevant for research applications in cancer biology, particularly in studies focusing on targeted therapies for tumors with BRAF mutations or EGFR dysregulation.
